Recent researches in triazole compounds as medicinal drugs.

Triazole compounds containing three nitrogen atoms in the five-membered aromatic azole ring are readily able to bind with a variety of enzymes and receptors in biological system via diverse non-covalent interactions, and thus display versatile biological activities. The related researches in triazole-based derivatives as medicinal drugs have been an extremely active topic, and numerous excellent achievements have been acquired. Noticeably, a large number of triazole compounds as clinical drugs or candidates have been frequently employed for the treatment of various types of diseases, which have shown their large development value and wide potential as medicinal agents. This work systematically reviewed the recent researches and developments of the whole range of triazole compounds as medicinal drugs, including antifungal, anticancer, antibacterial, antitubercular, antiviral, anti-inflammatory and analgesic, anticonvulsant, antiparasitic, antidiabetic, anti-obesitic, antihistaminic, anti-neuropathic, antihypertensive as well as other biological activities. The perspectives of the foreseeable future in the research and development of triazole-based compounds as medicinal drugs are also presented. It is hoped that this review will serve as a stimulant for new thoughts in the quest for rational designs of more active and less toxic triazole medicinal drugs.

[1]  A. Chambery,et al.  Modular approach to triazole-linked 1,6-α-D-oligomannosides to the discovery of inhibitors of Mycobacterium tuberculosis cell wall synthetase. , 2010, The Journal of organic chemistry.

[2]  Yoshiko Kagoshima,et al.  Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities. , 2008, Bioorganic & medicinal chemistry letters.

[3]  Jia Li,et al.  Expeditious preparation of triazole-linked glycolipids via microwave accelerated click chemistry and their electrochemical and biological assessments , 2010 .

[4]  J. Ham,et al.  Acid-catalyzed synthesis of 10-substituted triazolyl artemisinins and their growth inhibitory activity against various cancer cells. , 2010, Bioorganic & medicinal chemistry letters.

[5]  K. Parmar,et al.  Synthesis and biological activity of novel 1,3,5‐trisubstituted 1,2,4‐triazole derivatives , 2010 .

[6]  S. Emanuel,et al.  1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. , 2005, Journal of medicinal chemistry.

[7]  L. H. Hansen,et al.  A click chemistry approach to pleuromutilin conjugates with nucleosides or acyclic nucleoside derivatives and their binding to the bacterial ribosome. , 2008, Journal of medicinal chemistry.

[8]  Evaluation of substituted triazol-1-yl-pyrimidines as inhibitors of Bacillus anthracis acetohydroxyacid synthase. , 2010, Biochimica et biophysica acta.

[9]  G. Zhanel,et al.  Evaluation of amphiphilic aminoglycoside-peptide triazole conjugates as antibacterial agents. , 2010, Bioorganic & medicinal chemistry letters.

[10]  R. Linhardt,et al.  Synthesis and Biological Evaluation of Non-Hydrolizable 1,2,3-Triazole Linked Sialic Acid Derivatives as Neuraminidase Inhibitors. , 2009, European journal of organic chemistry.

[11]  T. Robak,et al.  Depsipeptide (FK228) as a novel histone deacetylase inhibitor: mechanism of action and anticancer activity. , 2007, Mini reviews in medicinal chemistry.

[12]  Giulio Rastelli,et al.  Structure-based design of potent aromatase inhibitors by high-throughput docking. , 2011, Journal of medicinal chemistry.

[13]  B. Tekwani,et al.  Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. , 2010, Journal of medicinal chemistry.

[14]  A. Kohara,et al.  Synthesis and biological evaluation of 3-biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles as novel glycine transporter 1 inhibitors. , 2011, Journal of medicinal chemistry.

[15]  K. Parang,et al.  Carboxylic acid and phosphate ester derivatives of fluconazole: synthesis and antifungal activities. , 2004, Bioorganic & medicinal chemistry.

[16]  P. Yogeeswari,et al.  Syntheses and biological evaluation of new triazole-spirochromone conjugates as inhibitors of Mycobacterium tuberculosis , 2011 .

[17]  David S Goodsell,et al.  1,2,3‐Triazole as a Peptide Surrogate in the Rapid Synthesis of HIV‐1 Protease Inhibitors , 2005, Chembiochem : a European journal of chemical biology.

[18]  A. Ajay,et al.  Application of Huisgen (3+2) cycloaddition reaction: synthesis of 1-(2,3-dihydrobenzofuran-2-yl-methyl [1,2,3]-triazoles and their antitubercular evaluations. , 2010, European journal of medicinal chemistry.

[19]  E. AUGUSTYNOWICZ-KOPEĆ,et al.  SYNTHESIS AND TUBERCULOSTATIC ACTIVITY OF NOVEL 1,2,4-TRIAZOLES OBTAINED FROM HETEROCYCLIC CARBOHYDRAZIDES , 2010 .

[20]  Liu Liu,et al.  Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity. , 2011, Journal of medicinal chemistry.

[21]  A. Oyelere,et al.  Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group. , 2008, Bioorganic & medicinal chemistry.

[22]  Beena,et al.  Synthesis and antibacterial activity evaluation of metronidazole-triazole conjugates. , 2009, Bioorganic & medicinal chemistry letters.

[23]  Ihsan A. Shehadi,et al.  Physicochemical properties of antifungal drug-cyclodextrin complexes prepared by supercritical carbon dioxide and by conventional techniques. , 2009, Journal of pharmaceutical and biomedical analysis.

[24]  A. Peksel,et al.  Synthesis in solvent-free conditions, characterization and biological activity of a new Schiff-base ligand and its Cu(II) complex , 2009 .

[25]  Z. Su,et al.  Syntheses and structures of organic-inorganic hybrid compounds based on metal-fluconazole coordination polymers and the beta-Mo8O26 anion. , 2007, Inorganic chemistry.

[26]  V. Gandin,et al.  Synthesis, characterization, and in vitro antitumor properties of tris(hydroxymethyl)phosphine copper(I) complexes containing the new bis(1,2,4-triazol-1-yl)acetate ligand. , 2006, Journal of medicinal chemistry.

[27]  Giovanni Sorba,et al.  Click chemistry reactions in medicinal chemistry: Applications of the 1,3‐dipolar cycloaddition between azides and alkynes , 2008, Medicinal research reviews.

[28]  T. Chou,et al.  Design, synthesis, and biological evaluation of novel water-soluble N-mustards as potential anticancer agents. , 2011, Bioorganic & medicinal chemistry.

[29]  M. Hemdan,et al.  Synthesis and Antimicrobial Study of 1,2,4-Triazole, Quinazoline and Benzothiazole Derivatives from 1-Naphthoylisothiocyanate , 2010 .

[30]  Y. Queneau,et al.  Synthesis of sugars embodying conjugated carbonyl systems and related triazole derivatives from carboxymethyl glycoside lactones. Evaluation of their antimicrobial activity and toxicity. , 2011, Bioorganic & medicinal chemistry.

[31]  C. Lee,et al.  C5-Modified nucleosides exhibiting anticancer activity. , 2009, Bioorganic & medicinal chemistry letters.

[32]  E. Durantini,et al.  Synthesis, spectroscopic properties and photodynamic activity of a novel Zn(II) phthalocyanine substituted by fluconazole groups , 2008 .

[33]  F. Pavón,et al.  Antiobesity effects of the novel in vivo neutral cannabinoid receptor antagonist 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole – LH 21 , 2006, Neuropharmacology.

[34]  P. Taylor,et al.  Conformational remodeling of femtomolar inhibitor-acetylcholinesterase complexes in the crystalline state. , 2010, Journal of the American Chemical Society.

[35]  Brendan L Wilkinson,et al.  Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides. , 2007, Journal of medicinal chemistry.

[36]  J. Neyts,et al.  Arylethynyltriazole acyclonucleosides inhibit hepatitis C virus replication. , 2008, Bioorganic & medicinal chemistry letters.

[37]  Jian Zhang,et al.  Developments of combretastatin A-4 derivatives as anticancer agents. , 2011, Current medicinal chemistry.

[38]  Z. Chohan,et al.  Synthesis, characterization and biological studies of oxovanadium(IV) complexes with triazole-derived Schiff bases , 2009 .

[39]  M. Du,et al.  Synthesis, crystal structures and in vitro anti-fungal activities of two silver(I) coordination polymers with fluconazole , 2007 .

[40]  M. Radi,et al.  Synthesis and biological evaluation of new enantiomerically pure azole derivatives as inhibitors of Mycobacterium tuberculosis. , 2009, Bioorganic & medicinal chemistry letters.

[41]  R. Hamatake,et al.  A Novel Nonnucleoside Analogue That Inhibits Human Immunodeficiency Virus Type 1 Isolates Resistant to Current Nonnucleoside Reverse Transcriptase Inhibitors , 2006, Antimicrobial Agents and Chemotherapy.

[42]  K. Parang,et al.  Click chemistry inspired one-pot synthesis of 1,4-disubstituted 1,2,3-triazoles and their Src kinase inhibitory activity. , 2011, Bioorganic & medicinal chemistry letters.

[43]  H. Rady,et al.  Synthesis of new acridines and hydrazones derived from cyclic beta-diketone for cytotoxic and antiviral evaluation. , 2009, European journal of medicinal chemistry.

[44]  G. Aktay,et al.  1-Acylthiosemicarbazides, 1,2,4-triazole-5(4H)-thiones, 1,3,4-thiadiazoles and hydrazones containing 5-methyl-2-benzoxazolinones: synthesis, analgesic-anti-inflammatory and antimicrobial activities. , 2007, Bioorganic & medicinal chemistry.

[45]  Yun Tang,et al.  Preparation of triazole-linked glycosylated α-ketocarboxylic acid derivatives as new PTP1B inhibitors. , 2011, Carbohydrate research.

[46]  V. Locatelli,et al.  Toward potent ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure. 2. Synthesis and pharmacological in vitro and in vivo evaluations. , 2007, Journal of medicinal chemistry.

[47]  P. Cheng,et al.  The coordination chemistry of Zn(II), Cd(II) and Hg(II) complexes with 1,2,4-triazole derivatives. , 2011, Dalton transactions.

[48]  M. Čuperlović-Culf,et al.  Synthesis and structure-activity relationship of 1- and 2-substituted-1,2,3-triazole letrozole-based analogues as aromatase inhibitors. , 2011, European journal of medicinal chemistry.

[49]  J. Chiva,et al.  1-Amido-1-phenyl-3-piperidinylbutanes--CCR5 antagonists for the treatment of HIV: part 2. , 2009, Bioorganic & medicinal chemistry letters.

[50]  Ji-Young Kim,et al.  Synthesis and structure-activity studies of novel homomorpholine oxazolidinone antibacterial agents. , 2009, Bioorganic & medicinal chemistry letters.

[51]  Osman A. B. S. M. Gani,et al.  1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin. , 2008, Bioorganic & medicinal chemistry.

[52]  C. Eyermann,et al.  Novel Substituted (Pyridin-3-yl)phenyloxazolidinones: Antibacterial Agents with Reduced Activity against Monoamine Oxidase A and Increased Solubility , 2007 .

[53]  X. Qian,et al.  The novel anti-tumor agents of 4-triazol-1,8-naphthalimides: synthesis, cytotoxicity, DNA intercalation and photocleavage. , 2011, European journal of medicinal chemistry.

[54]  Santhosh M. Samuel,et al.  Synthesis and antibacterial activity of new N-linked 5-triazolylmethyl oxazolidinones. , 2005, Bioorganic & medicinal chemistry.

[55]  Xingshu Li,et al.  Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors. , 2011, Bioorganic & medicinal chemistry.

[56]  N. Siddiqui,et al.  Synthesis, anticonvulsant and toxicity evaluation of 2-(1H-indol-3-yl)acetyl-N-(substituted phenyl)hydrazine carbothioamides and their related heterocyclic derivatives , 2008, Acta pharmaceutica.

[57]  P. T. Perumal,et al.  Regioselective synthesis and biological evaluation of bis(indolyl)methane derivatized 1,4-disubstituted 1,2,3-bistriazoles as anti-infective agents. , 2009, Bioorganic & medicinal chemistry letters.

[58]  J. Sangshetti,et al.  Synthesis of novel 3-(1-(1-substituted piperidin-4-yl)-1H-1,2,3-triazol-4-yl)-1,2,4-oxadiazol-5(4H)-one as antifungal agents. , 2009, Bioorganic & medicinal chemistry letters.

[59]  P. Murphy,et al.  Hybrid angiogenesis inhibitors: synthesis and biological evaluation of bifunctional compounds based on 1-deoxynojirimycin and aryl-1,2,3-triazoles. , 2008, Bioorganic & medicinal chemistry letters.

[60]  S. Patil,et al.  Synthesis, spectral characterization, in vitro antibacterial, antifungal and cytotoxic activities of Co(II), Ni(II) and Cu(II) complexes with 1,2,4-triazole Schiff bases. , 2008, European journal of medicinal chemistry.

[61]  S. Matsuoka,et al.  Synthesis and biological evaluation of triazole analogues of antillatoxin , 2011 .

[62]  Karunakaran A Kalesh,et al.  High-throughput discovery of Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) inhibitors using click chemistry. , 2009, Organic letters.

[63]  A. Kamal,et al.  Synthesis and biological evaluation of estradiol linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates as potential anticancer agents. , 2011, Bioorganic & medicinal chemistry.

[64]  Mohammad A. Hassan,et al.  Synthesis and Anticandidal Activity of Azole‐Containing Sulfonamides , 2008, Archiv der Pharmazie.

[65]  P. Rajakumar,et al.  Synthesis and in-vitro anti-inflammatory activity of novel glycodendrimers with benzene 1,3,5 carboxamide core and triazole as branching unit. , 2011, European journal of medicinal chemistry.

[66]  Q. Rao,et al.  The Hsp90 inhibitor 17-allylamide-17-demethoxygeldanamycin induces apoptosis and differentiation of Kasumi-1 harboring the Asn822Lys KIT mutation and down-regulates KIT protein level. , 2006, Leukemia research.

[67]  U. Nilsson,et al.  Synthesis of galactose-mimicking 1H-(1,2,3-triazol-1-yl)-mannosides as selective galectin-3 and 9N inhibitors. , 2007, Carbohydrate research.

[68]  Mahesh Uttamchandani,et al.  Rapid assembly and in situ screening of bidentate inhibitors of protein tyrosine phosphatases. , 2006, Organic letters.

[69]  Qingshan Zhang,et al.  Synthesis and antitumor activity of novel 2',3'-dideoxy-2',3'-diethanethionucleosides bearing 1,2,3-triazole residues. , 2010, Bioorganic & medicinal chemistry letters.

[70]  G. Gargala.  Drug treatment and novel drug target against Cryptosporidium. , 2008, Parasite.

[71]  Eiko Suzuki,et al.  Synthesis, cleavage, and antifungal activity of a number of novel, water-soluble ester prodrugs of antifungal triazole CS-758. , 2009, Bioorganic & medicinal chemistry letters.

[72]  M. Allan,et al.  Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase. , 2006, Bioorganic & medicinal chemistry letters.

[73]  Yun Ling,et al.  Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors. , 2011, Bioorganic & medicinal chemistry letters.

[74]  Keizo Yamashita,et al.  Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore. , 2007, Journal of medicinal chemistry.

[75]  C. Gill,et al.  Clubbed [1,2,3] triazoles by fluorine benzimidazole: a novel approach to H37Rv inhibitors as a potential treatment for tuberculosis. , 2008, Bioorganic & medicinal chemistry letters.

[76]  Qianjun Li,et al.  Synthesis of 1-beta-D-ribofuranosyl-3-ethynyl-[1,2,4]triazole and its in vitro and in vivo efficacy against Hantavirus. , 2008, Antiviral research.

[77]  D. Grigoriadis,et al.  Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists. , 2005, Journal of medicinal chemistry.

[78]  Qiang Zhang,et al.  Novel microtubule polymerization inhibitor with potent antiproliferative and antitumor activity. , 2009, Cancer research.

[79]  W. Denny,et al.  Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. , 2010, Journal of medicinal chemistry.

[80]  Guoqing Zhang,et al.  Enantioseparation of the New Antifungal Drug Iodiconazole and Structurally Related Triadimenol Analogues by CE with Neutral Cyclodextrin Additives , 2011 .

[81]  Andrea Scozzafava,et al.  Carbonic anhydrase IX: A new druggable target for the design of antitumor agents , 2008, Medicinal research reviews.

[82]  Kiran Singh,et al.  Synthesis, characterization and biological studies of Co(II), Ni(II), Cu(II) and Zn(II) complexes with bidentate Schiff bases derived by heterocyclic ketone. , 2006, European journal of medicinal chemistry.

[83]  Nathan T. Ross,et al.  An aldol-based build/couple/pair strategy for the synthesis of medium- and large-sized rings: discovery of macrocyclic histone deacetylase inhibitors. , 2010, Journal of the American Chemical Society.

[84]  J. M. Salas,et al.  In vitro and in vivo trypanocidal evaluation of nickel complexes with an azapurine derivative against Trypanosoma cruzi. , 2010, Journal of medicinal chemistry.

[85]  Haitao Ji,et al.  Design, Synthesis, and Antifungal Activity of Novel Conformationally Restricted Triazole Derivatives , 2009, Archiv der Pharmazie.

[86]  P. Workman,et al.  Targeting the Hsp90 chaperone: synthesis of novel resorcylic acid macrolactone inhibitors of Hsp90. , 2010, Chemistry.

[87]  B. Blagg,et al.  Click chemistry to probe Hsp90: Synthesis and evaluation of a series of triazole-containing novobiocin analogues. , 2010, Bioorganic & medicinal chemistry letters.

[88]  E. Assadpour,et al.  Design, synthesis, and antifungal activity of triazole and benzotriazole derivatives. , 2009, European journal of medicinal chemistry.

[89]  P. Gmeiner,et al.  1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands. , 2009, Journal of medicinal chemistry.

[90]  C. Jonsson,et al.  Structural effects on the phosphorylation of 3-substituted 1-β-d-ribofuranosyl-1,2,4-triazoles by human adenosine kinase , 2007, Bioorganic & Medicinal Chemistry Letters.

[91]  L. Hedstrom,et al.  Triazole inhibitors of Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase. , 2009, Journal of medicinal chemistry.

[92]  F. Seela,et al.  Nucleosides and oligonucleotides containing 1,2,3-triazole residues with nucleobase tethers: synthesis via the azide-alkyne 'click' reaction. , 2008, Bioorganic & medicinal chemistry.

[93]  Cheng‐He Zhou,et al.  Synthesis and activities of naphthalimide azoles as a new type of antibacterial and antifungal agents. , 2011, Bioorganic & medicinal chemistry letters.

[94]  R. Thieringer,et al.  Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1. , 2005, Bioorganic & medicinal chemistry letters.

[95]  K. Shah,et al.  Synthesis of Novel Indolyl‐1,2,4‐triazoles as Potent and Selective Anticancer Agents , 2011, Chemical biology & drug design.

[96]  Cheng‐He Zhou,et al.  Study on the synthesis and antimicrobial activity of novel cationic porphyrins , 2009 .

[97]  Jacobson,et al.  Polyamidoamine (PAMAM) dendrimer conjugates of "clickable" agonists of the A3 adenosine receptor and coactivation of the P2Y14 receptor by a tethered nucleotide. , 2010, Bioconjugate chemistry.

[98]  S. Patil,et al.  DNA cleavage and antimicrobial studies of 17-membered schiff base macrocyclic triazoles: synthesis and spectroscopic approach , 2010 .

[99]  Eiko Suzuki,et al.  Design, synthesis and antifungal activity of the novel water-soluble prodrug of antifungal triazole CS-758. , 2010, Chemical & pharmaceutical bulletin.

[100]  A. Gautier,et al.  Click Chelators – The Behavior of Platinum and Palladium Complexes in the Presence of Guanosine and DNA , 2010 .

[101]  Yihua Zhang,et al.  The anti-inflammatory effects of ZLJ-6, a novel dual cyclooxygenase/5-lipoxygenase inhibitor. , 2009, European journal of pharmacology.

[102]  Cheng‐He Zhou,et al.  Synthesis of Novel D-Glucose-derived Benzyl and Alkyl 1,2,3-Triazoles as Potential Antifungal and Antibacterial Agents , 2011 .

[103]  V. Calderone,et al.  Benzoyl and/or benzyl substituted 1,2,3-triazoles as potassium channel activators. VIII. , 2005, European journal of medicinal chemistry.

[104]  E. Tiekink,et al.  Antiviral evaluation of N-amino-1,2,3-triazoles against Cantagalo virus replication in cell culture. , 2009, European journal of medicinal chemistry.

[105]  E. Garvey,et al.  The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore. , 2009, Bioorganic & medicinal chemistry letters.

[106]  A. Malm,et al.  Synthesis and antimicrobial and pharmacological properties of new thiosemicarbazide and 1,2,4-triazole derivatives , 2011 .

[107]  V. Ferreira,et al.  Synthesis and anti-HSV-1 activity of new 1,2,3-triazole derivatives. , 2011, Bioorganic & medicinal chemistry.

[108]  I. Carvalho,et al.  'Click chemistry' synthesis of a library of 1,2,3-triazole-substituted galactose derivatives and their evaluation against Trypanosoma cruzi and its cell surface trans-sialidase. , 2010, Bioorganic & medicinal chemistry.

[109]  A. K. Saxsena,et al.  Ring A structural modified derivatives of withaferin A and the evaluation of their cytotoxic potential , 2011, Steroids.

[110]  M. P. Lynch,et al.  Comparative structure-activity relationship studies of 1-(5-methylsulfonylpyrid-2-yl)-5-alkyl and (hetero)aryl triazoles and pyrazoles in canine COX inhibition. , 2008, Bioorganic & medicinal chemistry letters.

[111]  Monika Gupta.  Efficient synthesis of antifungal active 9-substituted-3-aryl-5H,13aH-quinolino[3,2-f][1,2,4]triazolo[4,3-b][1,2,4]triazepines in ionic liquids. , 2011, Bioorganic & medicinal chemistry letters.

[112]  Qiang Zhang,et al.  Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways. , 2009, Bioorganic & medicinal chemistry.

[113]  Santhosh M. Samuel,et al.  Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones. , 2007, European journal of medicinal chemistry.

[114]  A. Olson,et al.  Rapid discovery and structure-activity profiling of novel inhibitors of human immunodeficiency virus type 1 protease enabled by the copper(I)-catalyzed synthesis of 1,2,3-triazoles and their further functionalization. , 2006, Journal of medicinal chemistry.

[115]  A. De Sarro,et al.  New triazoles and echinocandins: mode of action, in vitro activity and mechanisms of resistance , 2009, Expert review of anti-infective therapy.

[116]  Jun-min Zhou,et al.  Synthesis and biological evaluation of 4-aryl-5-cyano-2H-1,2,3-triazoles as inhibitor of HER2 tyrosine kinase. , 2007, Bioorganic & medicinal chemistry.

[117]  S. Ghosh,et al.  Design, synthesis and bioactivity of catechin/epicatechin and 2-azetidinone derived chimeric molecules. , 2009, Bioorganic & medicinal chemistry letters.

[118]  A. Frassetto,et al.  Pharmacological evaluation of LH-21, a newly discovered molecule that binds to cannabinoid CB1 receptor. , 2008, European journal of pharmacology.

[119]  Y. Ünver,et al.  Spectroscopic and theoretical study of 1,2,4-triazole-3-one based salicylaldimine complexes and evaluation of superoxide-scavenging properties , 2009 .

[120]  G. Gores,et al.  Clinical Trial of the Pan‐Caspase Inhibitor, IDN‐6556, in Human Liver Preservation Injury , 2007, American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons.

[121]  Wang Yan,et al.  Recent advances in the researches of triazole compounds as medicinal drugs , 2011 .

[122]  Carlos R Rodrigues,et al.  Synthesis, tuberculosis inhibitory activity, and SAR study of N-substituted-phenyl-1,2,3-triazole derivatives. , 2006, Bioorganic & medicinal chemistry.

[123]  Sadanandam Palle,et al.  Synthesis and cytotoxicity evaluation of novel 1,4-disubstituted 1,2,3-triazoles via CuI catalysed 1,3-dipolar cycloaddition. , 2010, European journal of medicinal chemistry.

[124]  N. Khalil.  Efficient synthesis of novel 1,2,4-triazole fused acyclic and 21-28 membered macrocyclic and/or lariat macrocyclic oxaazathia crown compounds with potential antimicrobial activity. , 2010, European journal of medicinal chemistry.

[125]  P. Murphy,et al.  Biological study of the Angiogenesis Inhibitor N‐(8‐(3‐ethynylphenoxy)octyl‐1‐deoxynojirimycin , 2010, Chemical biology & drug design.

[126]  J. Heeres,et al.  Synthesis and in vitro and in vivo Antifungal Activity of the Hydroxy Metabolites of Saperconazole , 2010, ChemMedChem.

[127]  E. Zangrando,et al.  1-(2-Picolyl)-substituted 1,2,3-triazole as novel chelating ligand for the preparation of ruthenium complexes with potential anticancer activity. , 2011, Dalton transactions.

[128]  C. Gill,et al.  SAR study of clubbed [1,2,4]-triazolyl with fluorobenzimidazoles as antimicrobial and antituberculosis agents. , 2009, European journal of medicinal chemistry.

[129]  P. Plas,et al.  3-Thio-1,2,4-triazoles, novel somatostatin sst2/sst5 agonists. , 2005, Bioorganic & medicinal chemistry letters.

[130]  S. Béni,et al.  Cyclodextrin/imatinib complexation: binding mode and charge dependent stabilities. , 2007, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[131]  Rongmei Geng,et al.  Synthesis, Antibacterial and Antifungal Activities of Novel 1,2,4‐Triazolium Derivatives , 2009, Archiv der Pharmazie.

[132]  G. V. Suresh Kumar,et al.  Synthesis of new 4-isopropylthiazole hydrazide analogs and some derived clubbed triazole, oxadiazole ring systems--a novel class of potential antibacterial, antifungal and antitubercular agents. , 2009, European journal of medicinal chemistry.

[133]  C. O. Mellet,et al.  Multi-mannosides based on a carbohydrate scaffold: synthesis, force field development, molecular dynamics studies, and binding affinities for lectin Con A. , 2007, The Journal of organic chemistry.

[134]  G. Kumar,et al.  NMR and molecular modelling studies on the interaction of fluconazole with β-cyclodextrin , 2009, Chemistry Central journal.

[135]  B. Tucer,et al.  The effect of chloroquine treatment in malignant astrocytomas on prognosis , 2013 .

[136]  Shabana I. Khan,et al.  Synthesis of 4‐aminoquinoline‐1,2,3‐triazole and 4‐aminoquinoline‐1,2,3‐triazole‐1,3,5‐triazine Hybrids as Potential Antimalarial Agents , 2011, Chemical biology & drug design.

[137]  M. Bhat,et al.  Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues. , 2009, Bioorganic & medicinal chemistry letters.

[138]  A. B. Pierini,et al.  Design, Synthesis and 3-D Characterization of 1-Benzenesulfonyl-1,2,3,4- Tetrahydroquinolines as Lead Scaffold for Antiparasitic Drug , 2010 .

[139]  M. Suresh,et al.  An overview of tuberculosis chemotherapy - a literature review. , 2011, Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques.

[140]  P. Zoumpoulakis,et al.  Sulfonamide-1,2,4-triazole derivatives as antifungal and antibacterial agents: synthesis, biological evaluation, lipophilicity, and conformational studies. , 2008, Bioorganic & medicinal chemistry.

[141]  E. De Clercq,et al.  Synthesis of some novel thiourea derivatives obtained from 5-[(4-aminophenoxy)methyl]-4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones and evaluation as antiviral/anti-HIV and anti-tuberculosis agents. , 2008, European journal of medicinal chemistry.

[142]  Xiaochen Wang,et al.  Synthesis of 4β-triazole-podophyllotoxin derivatives by azide-alkyne cycloaddition and biological evaluation as potential antitumor agents. , 2011, European journal of medicinal chemistry.

[143]  H. Kung,et al.  Quick assembly of 1,4-diphenyltriazoles as probes targeting beta-amyloid aggregates in Alzheimer's disease. , 2007, Journal of medicinal chemistry.

[144]  W. L. Jorgensen,et al.  A remote arene-binding site on prostate specific membrane antigen revealed by antibody-recruiting small molecules. , 2010, Journal of the American Chemical Society.

[145]  M. Baba,et al.  Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety. , 2006, Journal of medicinal chemistry.

[146]  H. Kumar,et al.  1,3,4-Oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid: synthesis and preliminary evaluation of biological properties. , 2008, European journal of medicinal chemistry.

[147]  B. M. Pinto,et al.  Carbocycles related to oseltamivir as influenza virus group-1-specific neuraminidase inhibitors. Binding to N1 enzymes in the context of virus-like particles. , 2010, Journal of medicinal chemistry.

[148]  Grant W. Brown,et al.  New azole antifungal agents with novel modes of action: synthesis and biological studies of new tridentate ligands based on pyrazole and triazole. , 2011, European journal of medicinal chemistry.

[149]  C. Eyermann,et al.  Identification of 4-substituted 1,2,3-triazoles as novel oxazolidinone antibacterial agents with reduced activity against monoamine oxidase A. , 2005, Journal of medicinal chemistry.

[150]  U. Egerland,et al.  New GABA-modulating 1,2,4-oxadiazole derivatives and their anticonvulsant activity. , 2007, European journal of medicinal chemistry.

[151]  Honggang Hu,et al.  Synthesis and antifungal evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase. , 2010, European journal of medicinal chemistry.

[152]  K. Hostetler,et al.  Application of kinase bypass strategies to nucleoside antivirals. , 2011, Antiviral research.

[153]  D. Klepacki,et al.  Binding and Action of CEM-101, a New Fluoroketolide Antibiotic That Inhibits Protein Synthesis , 2010, Antimicrobial Agents and Chemotherapy.

[154]  E. Monte,et al.  Thiourea, triazole and thiadiazine compounds and their metal complexes as antifungal agents. , 2005, Journal of inorganic biochemistry.

[155]  A. Llebaria,et al.  Click chemistry approach to new N-substituted aminocyclitols as potential pharmacological chaperones for Gaucher disease. , 2010, Journal of medicinal chemistry.

[156]  M. Gouda,et al.  Synthesis and study of some new 1,3-isoindoledione derivatives as potential antibacterial agents. , 2010, European journal of medicinal chemistry.

[157]  Xiaoguang Lei,et al.  Efficient Synthesis of a Novel Resorcyclide as Anticancer Agent Based on Hsp90 Inhibition. , 2008, Advanced synthesis & catalysis.

[158]  J. McKerrow,et al.  Identification of a new class of nonpeptidic inhibitors of cruzain. , 2008, Journal of the American Chemical Society.

[159]  K. Jacobson,et al.  2-Dialkynyl derivatives of (N)-methanocarba nucleosides: 'Clickable' A(3) adenosine receptor-selective agonists. , 2010, Bioorganic & medicinal chemistry.

[160]  A. Timerbaev,et al.  Structure-activity relationships for NAMI-A-type complexes (HL)[trans-RuCl4L(S-dmso)ruthenate(III)] (L = imidazole, indazole, 1,2,4-triazole, 4-amino-1,2,4-triazole, and 1-methyl-1,2,4-triazole): aquation, redox properties, protein binding, and antiproliferative activity. , 2007, Journal of medicinal chemistry.

[161]  M. Deshpande,et al.  Exploration of click reaction for the synthesis of modified nucleosides as chitin synthase inhibitors. , 2009, Bioorganic & medicinal chemistry.

[162]  V. Belakhov,et al.  Design, synthesis, and evaluation of novel fluoroquinolone-aminoglycoside hybrid antibiotics. , 2009, Journal of medicinal chemistry.

[163]  Jun O. Liu,et al.  Synthesis of Oleanolic Acid Dimers as Inhibitors of Glycogen Phosphorylase , 2010, Chemistry & biodiversity.

[164]  Honggang Hu,et al.  Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols. , 2009, Bioorganic & medicinal chemistry letters.

[165]  G. Krishnamurthy,et al.  Small molecule inhibitors of HIV RT Ribonuclease H. , 2010, Bioorganic & medicinal chemistry letters.

[166]  A. V. Adhikari,et al.  New quinolin-4-yl-1,2,3-triazoles carrying amides, sulphonamides and amidopiperazines as potential antitubercular agents. , 2011, European journal of medicinal chemistry.

[167]  Courtney C Aldrich,et al.  Inhibition of siderophore biosynthesis by 2-triazole substituted analogues of 5'-O-[N-(salicyl)sulfamoyl]adenosine: antibacterial nucleosides effective against Mycobacterium tuberculosis. , 2008, Journal of medicinal chemistry.

[168]  G. Besra,et al.  Identification of arylamine N-acetyltransferase inhibitors as an approach towards novel anti-tuberculars , 2010, Protein & Cell.

[169]  S. Srivastava,et al.  Betulinic acid derivatives as anticancer agents: structure activity relationship. , 2006, Anti-cancer agents in medicinal chemistry.

[170]  C. K. Andrade,et al.  The evaluation of quinonoid compounds against Trypanosoma cruzi: synthesis of imidazolic anthraquinones, nor-beta-lapachone derivatives and beta-lapachone-based 1,2,3-triazoles. , 2010, Bioorganic & medicinal chemistry.

[171]  A. Basu,et al.  Glycosidase inhibition by 1-glycosyl-4-phenyl triazoles. , 2005, Bioorganic & medicinal chemistry letters.

[172]  Wei Zhang,et al.  Microwave-assisted construction of triazole-linked amino acid–glucoside conjugates as novel PTP1B inhibitors , 2011 .

[173]  J. Neyts,et al.  S-aryltriazole acyclonucleosides: synthesis and biological evaluation against hepatitis C virus. , 2010, Bioorganic & medicinal chemistry letters.

[174]  Cheng‐He Zhou,et al.  Synthesis of Azole-containing Piperazine Derivatives and Evaluation of their Antibacterial, Antifungal and Cytotoxic Activities , 2010 .

[175]  R. Thieringer,et al.  4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. , 2008, Bioorganic & medicinal chemistry letters.

[176]  Yan Zou,et al.  Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents. , 2011, Bioorganic & medicinal chemistry letters.

[177]  Amanda C. Engler,et al.  Effects of side group functionality and molecular weight on the activity of synthetic antimicrobial polypeptides. , 2011, Biomacromolecules.

[178]  Y. Sham,et al.  Triazole-linked inhibitors of inosine monophosphate dehydrogenase from human and Mycobacterium tuberculosis. , 2010, Journal of medicinal chemistry.

[179]  E. Durantini,et al.  The photodynamic activity of a novel porphyrin derivative bearing a fluconazole structure in different media and against Candida albicans , 2010 .

[180]  J. Iovanna,et al.  Novel triazole ribonucleoside down-regulates heat shock protein 27 and induces potent anticancer activity on drug-resistant pancreatic cancer. , 2009, Journal of medicinal chemistry.

[181]  K. Chai,et al.  Synthesis of 2-substituted-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazoles as potential anticonvulsant agents , 2009, Archives of pharmacal research.

[182]  M. Uttamchandani,et al.  Rapid assembly of matrix metalloprotease inhibitors using click chemistry. , 2006, Organic letters.

[183]  Y. Na.  Synthesis and Activity of Novel 1-Halogenobenzylindole Linked Triazole Derivatives as Antifungal Agents , 2011 .

[184]  Yan Zou,et al.  Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives. , 2011, European journal of medicinal chemistry.

[185]  Cheng‐He Zhou,et al.  Synthesis of Novel Halobenzyloxy and Alkoxy 1,2,4-Triazoles and Evaluation for Their Antifungal and Antibacterial Activities , 2010 .

[186]  Xiao‐Ming Li,et al.  Triazole and dihydroimidazole alkaloids from the marine sediment-derived fungus Penicillium paneum SD-44. , 2011, Journal of natural products.

[187]  Min Ju Kim,et al.  Synthesis and structure-activity relationship of 1,2,4-triazole-containing diarylpyrazolyl carboxamide as CB1 cannabinoid receptor-ligand. , 2010, Bioorganic & medicinal chemistry.

[188]  Gabriela Chiosis,et al.  Discovery and development of heat shock protein 90 inhibitors. , 2009, Bioorganic & medicinal chemistry.

[189]  Cheng‐He Zhou,et al.  Recent Researches in Metal Supramolecular Complexes as Anticancer Agents. , 2010, Anti-cancer agents in medicinal chemistry.

[190]  O. Phillips,et al.  Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones. , 2009, European journal of medicinal chemistry.

[191]  W. Goddard,et al.  Novel purine-based fluoroaryl-1,2,3-triazoles as neuroprotecting agents: synthesis, neuronal cell culture investigations, and CDK5 docking studies. , 2011, Bioorganic & medicinal chemistry letters.

[192]  Yiyi Zhang,et al.  Review on supermolecules as chemical drugs , 2009, Science in China. Series B, Chemistry.

[193]  A. Al-Bakri,et al.  Synthesis and antimicrobial activity of new 1,2,4-triazole-3-thiol metronidazole derivatives , 2010 .

[194]  A. Zhang,et al.  N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators , 2011 .

[195]  Cheng‐He Zhou,et al.  Synthesis of novel fluconazoliums and their evaluation for antibacterial and antifungal activities. , 2011, European journal of medicinal chemistry.

[196]  M. Cascante,et al.  Synthesis and structure-activity relationship study of novel cytotoxic carbamate and N-acylheterocyclic bearing derivatives of betulin and betulinic acid. , 2010, Bioorganic & medicinal chemistry.

[197]  P. Souza,et al.  Chemistry, antiproliferative activity and low nephrotoxicity of 3,5-diacetyl-1,2,4-triazol bis(4N-thiosemicarbazone) ligands and their platinum(II) complexes. , 2010, Dalton Transactions.

[198]  R. Uddin,et al.  Synthesis, antioxidant activities and urease inhibition of some new 1,2,4-triazole and 1,3,4-thiadiazole derivatives. , 2010, European journal of medicinal chemistry.

[199]  Sharad K. Pasale,et al.  Synthesis and biological evaluation of new 2-chloro-3-((4-phenyl-1H-1,2,3-triazol-1-yl)methyl)quinoline derivatives via click chemistry approach. , 2010, European journal of medicinal chemistry.

[200]  Cheng‐He Zhou,et al.  Synthesis and biological activities of novel amine-derived bis-azoles as potential antibacterial and antifungal agents. , 2010, European journal of medicinal chemistry.

[201]  C. Mercurio,et al.  Triazole-modified histone deacetylase inhibitors as a rapid route to drug discovery. , 2008, Journal of combinatorial chemistry.

[202]  K. Parang,et al.  Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities. , 2011, Bioorganic & medicinal chemistry letters.

[203]  J. Iovanna,et al.  Ligand-mediated highly effective and selective C-N coupling for synthesizing bioactive N-aryltriazole acyclonucleosides. , 2010, Organic letters.

[204]  M. D. Gao,et al.  Regulation of HSP27 on NF-κB pathway activation may be involved in metastatic hepatocellular carcinoma cells apoptosis , 2009, BMC Cancer.

[205]  Lynn Rasmussen,et al.  Antituberculosis activity of the molecular libraries screening center network library. , 2009, Tuberculosis.

[206]  S. McAlpine,et al.  Histone deacetylase inhibitors: synthesis of cyclic tetrapeptides and their triazole analogs , 2010 .

[207]  Sanghee Kim,et al.  Synthesis and Evaluation of 1,2,3-Triazole Containing Analogues of the Immunostimulant α-GalCer , 2007 .

[208]  O. Küçükbasmacı,et al.  Synthesis and antimicrobial activity evaluation of new 1,2,4-triazoles and 1,3,4-thiadiazoles bearing imidazo[2,1-b]thiazole moiety. , 2010, European journal of medicinal chemistry.

[209]  A. K. Atia.  Synthesis and Antibacterial Activities of New Metronidazole and Imidazole Derivatives , 2009, Molecules.

[210]  C. O. Mellet,et al.  1,2,3-Triazoles and related glycoconjugates as new glycosidase inhibitors , 2005 .

[211]  K. Ang,et al.  Nonpeptidic tetrafluorophenoxymethyl ketone cruzain inhibitors as promising new leads for Chagas disease chemotherapy. , 2010, Journal of medicinal chemistry.

[212]  M. Tegoni,et al.  Thioamido coordination in a thioxo-1,2,4-triazole copper(II) complex enhances nonapoptotic programmed cell death associated with copper accumulation and oxidative stress in human cancer cells. , 2007, Journal of medicinal chemistry.

[213]  E. Chaikof,et al.  Janus-type dendrimer-like poly(ethylene oxide)s. , 2008, Journal of the American Chemical Society.

[214]  S. Chattopadhyay,et al.  Synthesis and biological evaluation of bile acid dimers linked with 1,2,3-triazole and bis-beta-lactam. , 2008, Organic & biomolecular chemistry.

[215]  V. Locatelli,et al.  Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1. , 2007, Journal of medicinal chemistry.

[216]  H. Abdel-Rahman,et al.  Design, synthesis and molecular modeling study of acylated 1,2,4-triazole-3-acetates with potential anti-inflammatory activity. , 2009, European journal of medicinal chemistry.

[217]  A. Kamal,et al.  Synthesis and anticancer activity of chalcone-pyrrolobenzodiazepine conjugates linked via 1,2,3-triazole ring side-armed with alkane spacers. , 2011, European journal of medicinal chemistry.

[218]  B. Tekwani,et al.  Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. , 2010, Bioorganic & medicinal chemistry.

[219]  Wei Wang,et al.  Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists. , 2009, Bioorganic & medicinal chemistry letters.

[220]  S. Levy,et al.  N-hydroxybenzimidazole inhibitors of the transcription factor LcrF in Yersinia: novel antivirulence agents. , 2009, Journal of medicinal chemistry.

[221]  Yuan-Ying Jiang,et al.  In vitro and in vivo activities of HQQ-3, a new triazole antifungal agent. , 2006, Biological & pharmaceutical bulletin.

[222]  L. Goldani,et al.  Novel triazole antifungal drugs: focus on isavuconazole, ravuconazole and albaconazole. , 2010, Current opinion in investigational drugs.

[223]  P. Sharma,et al.  Advances in synthetic approach to and antifungal activity of triazoles , 2011, Beilstein journal of organic chemistry.

[224]  Yue Zhao,et al.  Anti-inflammatory effects and gastrointestinal safety of NNU-hdpa, a novel dual COX/5-LOX inhibitor. , 2009, European journal of pharmacology.

[225]  Â. Pinto,et al.  Novel 1,2,3-triazole derivatives for use against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain. , 2011, Journal of medicinal chemistry.

[226]  Design, Synthesis, and Biological Evaluation of 1,5‐Diaryl‐1,2,4‐triazole Derivatives as Selective Cyclooxygenase‐2 Inhibitors , 2010, Archiv der Pharmazie.

[227]  R. Schibli,et al.  Novel glycated [99mTc(CO)3]-labeled bombesin analogues for improved targeting of gastrin-releasing peptide receptor-positive tumors. , 2008, Bioconjugate chemistry.

[228]  Haladhar Dev Sarma,et al.  Preparation and preliminary bioevaluation of 99mTc(CO)3-11β-progesterone derivative prepared via click chemistry route. , 2010, Nuclear medicine and biology.

[229]  V. Chaturvedi,et al.  Novel aryloxy azolyl chalcones with potent activity against Mycobacterium tuberculosis H37Rv. , 2011, European journal of medicinal chemistry.

[230]  A. Saxena,et al.  Studies on novel 4β-[(4-substituted)-1,2,3-triazol-1-yl] podophyllotoxins as potential anticancer agents , 2008 .

[231]  P. Shukla,et al.  Tetrahydronaphthyl azole oxime ethers: the conformationally rigid analogues of oxiconazole as antibacterials. , 2009, European journal of medicinal chemistry.

[232]  S. Yee,et al.  Synthesis and CYP26A1 inhibitory activity of 1-[benzofuran-2-yl-(4-alkyl/aryl-phenyl)-methyl]-1H-triazoles. , 2006, Bioorganic & medicinal chemistry.

[233]  Cheng‐He Zhou,et al.  Synthesis, antibacterial and antifungal activities of some carbazole derivatives. , 2010, Bioorganic & medicinal chemistry letters.

[234]  J. Stein,et al.  Structure-Activity Relationships of Diverse Oxazolidinones for Linezolid-Resistant Staphylococcus aureus Strains Possessing the cfr Methyltransferase Gene or Ribosomal Mutations , 2010, Antimicrobial Agents and Chemotherapy.

[235]  Eric Oldfield,et al.  Amiodarone has intrinsic anti-Trypanosoma cruzi activity and acts synergistically with posaconazole. , 2006, Journal of medicinal chemistry.

[236]  A. V. Adhikari,et al.  Synthesis and antimicrobial activities of novel quinoline derivatives carrying 1,2,4-triazole moiety. , 2009, European journal of medicinal chemistry.

[237]  Juan Li,et al.  Anti-Inflammatory and Analgesic Potency of Carboxyamidotriazole, a Tumorostatic Agent , 2008, Journal of Pharmacology and Experimental Therapeutics.

[238]  V. Křen,et al.  Synthesis and biological activity of glycosyl-1H-1,2,3-triazoles. , 2010, Bioorganic & medicinal chemistry letters.

[239]  A. Demirbaş,et al.  Synthesis of some new biheterocyclic triazole derivatives and evaluation of their antimicrobial activity , 2010, Turkish Journal of Chemistry.

[240]  A. Kozikowski,et al.  Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. , 2010, Journal of medicinal chemistry.

[241]  E. S. Coimbra,et al.  Thiopurine derivatives containing triazole and steroid: synthesis, antimalarial and antileishmanial activities. , 2011, Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie.

[242]  Anurag Chaudhary,et al.  Combretastatin a-4 analogs as anticancer agents. , 2007, Mini reviews in medicinal chemistry.

[243]  S. Luthra,et al.  Synthesis and in vitro evaluation of [18F]fluoroethyl triazole labelled [Tyr3]octreotate analogues using click chemistry. , 2011, Bioorganic & Medicinal Chemistry Letters.

[244]  M. Rejžek,et al.  Synthesis of alpha- and beta-D-glucopyranosyl triazoles by CuAAC 'click chemistry': reactant tolerance, reaction rate, product structure and glucosidase inhibitory properties. , 2010, Carbohydrate research.

[245]  Giuseppe Bifulco,et al.  A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistry. , 2010, Journal of medicinal chemistry.

[246]  N. Siddiqui,et al.  Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening. , 2010, European journal of medicinal chemistry.

[247]  Cheng-He Zhou,et al.  Synthesis of novel sulfanilamide-derived 1,2,3-triazoles and their evaluation for antibacterial and antifungal activities. , 2010, European journal of medicinal chemistry.

[248]  V. Calderone,et al.  1,4- and 2,4-substituted-1,2,3-triazoles as potential potassium channel activators. VII. , 2005, Farmaco.

[249]  H. Mahmoud,et al.  Applications of 2-arylhydrazononitriles in synthesis: preparation of new indole containing 1,2,3-triazole, pyrazole and pyrazolo[1,5-a]pyrimidine derivatives and evaluation of their antimicrobial activities. , 2011, European journal of medicinal chemistry.

[250]  Zoran Radić,et al.  In situ selection of lead compounds by click chemistry: target-guided optimization of acetylcholinesterase inhibitors. , 2005, Journal of the American Chemical Society.

[251]  V. Pore,et al.  Synthesis and antimicrobial activity of beta-lactam-bile acid conjugates linked via triazole. , 2008, Bioorganic & medicinal chemistry letters.

[252]  Min Zhang,et al.  Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking. , 2006, Journal of medicinal chemistry.

[253]  N. Patel,et al.  Pharmacological evaluation and characterizations of newly synthesized 1,2,4-triazoles. , 2010, European journal of medicinal chemistry.

[254]  C. Kaiser,et al.  Synthesis, biological activity, and molecular modeling studies of 1H-1,2,3-triazole derivatives of carbohydrates as alpha-glucosidases inhibitors. , 2010, Journal of medicinal chemistry.

[255]  E. Laurini,et al.  2‐Aryl‐3‐(1H‐Azol‐1‐yl)‐1H‐Indole Derivatives: A New Class of Antimycobacterial Compounds – Conventional Heating in Comparison with MW‐Assisted Synthesis , 2009, Archiv der Pharmazie.

[256]  Maxwell M. Reeve,et al.  Synthesis of an Antibacterial Compound Containing a 1,4-Substituted 1H-1,2,3-Triazole: A Scaleable Alternative to the “Click” Reaction , 2010 .

[257]  J. Gut,et al.  Comparison of the antiplasmodial and falcipain-2 inhibitory activity of beta-amino alcohol thiolactone-chalcone and isatin-chalcone hybrids. , 2010, Bioorganic & medicinal chemistry letters.

[258]  E. LaVoie,et al.  Novel topoisomerase I-targeting antitumor agents synthesized from the N,N,N-trimethylammonium derivative of ARC-111, 5H-2,3-dimethoxy-8,9-methylenedioxy-5-[(2-N,N,N-trimethylammonium)ethyl]dibenzo[c,h][1,6]naphthyridin-6-one iodide. , 2008, European journal of medicinal chemistry.

[259]  A. Doucette,et al.  New carbon-linked azole oxazolidinones with improved potency and pharmacokinetics. , 2007, Bioorganic & medicinal chemistry letters.

[260]  K. V. Sujith,et al.  Regioselective reaction: synthesis and pharmacological study of Mannich bases containing ibuprofen moiety. , 2009, European journal of medicinal chemistry.

[261]  A. Mavrova,et al.  Synthesis, cytotoxicity and effects of some 1,2,4-triazole and 1,3,4-thiadiazole derivatives on immunocompetent cells. , 2009, European journal of medicinal chemistry.

[262]  J. Ryu,et al.  A rapid synthesis of lavendustin-mimetic small molecules by click fragment assembly. , 2010, Bioorganic & medicinal chemistry letters.

[263]  V. Kulkarni,et al.  Microwave assisted synthesis of potential anti infective and anticonvulsant thiosemicarbazones. , 2009 .

[264]  I. Chaiken,et al.  Introducing metallocene into a triazole peptide conjugate reduces its off‐rate and enhances its affinity and antiviral potency for HIV‐1 gp120 , 2009, Journal of molecular recognition : JMR.

[265]  L. Naesens,et al.  Application of the phosphoramidate ProTide approach to the antiviral drug ribavirin , 2008, Bioorganic & Medicinal Chemistry.

[266]  Qiuye Wu,et al.  Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents. , 2008, Bioorganic & medicinal chemistry letters.

[267]  A. Felton,et al.  New global recommendations: a multidisciplinary approach to improving outcomes in diabetes. , 2007, Primary care diabetes.

[268]  Z. Chohan,et al.  Metal based biologically active compounds: design, synthesis, and antibacterial/antifungal/cytotoxic properties of triazole-derived Schiff bases and their oxovanadium(IV) complexes. , 2010, European journal of medicinal chemistry.

[269]  J. Chen,et al.  Synthesis and anticonvulsant evaluation of 4-(4-alkoxylphenyl)-3-ethyl-4H-1,2,4-triazoles as open-chain analogues of 7-alkoxyl-4,5-dihydro[1,2,4]triazolo[4,3-a]quinolines. , 2007, Bioorganic & medicinal chemistry.

[270]  B. Potter,et al.  Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template. , 2010, Journal of medicinal chemistry.

[271]  B. Torbett,et al.  A copper(I)-catalyzed 1,2,3-triazole azide-alkyne click compound is a potent inhibitor of a multidrug-resistant HIV-1 protease variant. , 2008, Journal of medicinal chemistry.

[272]  Keith Tan,et al.  The effects of hepatic impairment on the pharmacokinetics of fosfluconazole and fluconazole following a single intravenous bolus injection of fosfluconazole. , 2004, British journal of clinical pharmacology.

[273]  Cheng‐He Zhou,et al.  Synthesis and their evaluation for their antimicrobial activity of diphenyl piperazine-based sulfanilamides , 2011 .

[274]  K. Jacobson,et al.  GPCR ligand dendrimer (GLiDe) conjugates: adenosine receptor interactions of a series of multivalent xanthine antagonists. , 2011, Bioconjugate chemistry.

[275]  P. Jänne,et al.  Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors , 2011, ACS medicinal chemistry letters.

[276]  N. Sewald,et al.  "Clicktophycin-52": a bioactive cryptophycin-52 triazole analogue. , 2010, Organic letters.

[277]  Mamdouh M. Ali,et al.  Synthesis of New Quinoline Derivatives as Inhibitors of Human Tumor Cells Growth , 2010, Archiv der Pharmazie.

[278]  S. Yee,et al.  Potent CYP19 (aromatase) 1-[(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: synthesis and biological evaluation. , 2006, Journal of medicinal chemistry.

[279]  B. Poojary,et al.  Synthesis, antimicrobial and anti-inflammatory activities of some 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 1,2,4-triazolo[3,4-b][1,3,4]thiadiazines bearing trichlorophenyl moiety. , 2008, European journal of medicinal chemistry.

[280]  Abbas Shafiee,et al.  Design, synthesis, and biological evaluation of substituted 3-alkylthio-4,5-diaryl-4H-1,2,4-triazoles as selective COX-2 inhibitors. , 2006, Bioorganic & medicinal chemistry.

[281]  N. Patil,et al.  Synthesis, Characterization and Biological Activities of Cu(II), Co(II), Ni(II), Mn(II) and Fe(III) Complexes with Schiff Base Derived from 3-(4-Chlorophenoxymethyl)-4-amino-5-mercapto-1,2,4-triazole , 2008 .

[282]  P. Le Pape,et al.  Design, synthesis, and evaluation of 1-(N-benzylamino)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents. , 2008, Bioorganic & medicinal chemistry letters.

[283]  R. Thieringer,et al.  Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. , 2008, Bioorganic & medicinal chemistry letters.

[284]  Saskia Nijmeijer,et al.  Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity. , 2011, Journal of medicinal chemistry.

[285]  Gergo Nagy,et al.  Synthesis of variously coupled conjugates of D-glucose, 1,3,4-oxadiazole, and 1,2,3-triazole for inhibition of glycogen phosphorylase. , 2011, Carbohydrate research.

[286]  B. Blagg,et al.  Synthesis and evaluation of coumermycin A1 analogues that inhibit the Hsp90 protein folding machinery. , 2006, Organic letters.

[287]  N. Sach,et al.  Development of Scalable Syntheses of Selective PI3K inhibitors , 2011 .

[288]  V. Kanase,et al.  Studying synergism of methyl linked cyclohexyl thiophenes with triazole: synthesis and their cdk5/p25 inhibition activity. , 2011, European journal of medicinal chemistry.

[289]  E. Kuepeli,et al.  Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity. , 2007, Bioorganic & medicinal chemistry.

[290]  R. Mach,et al.  Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay. , 2011, Bioorganic & medicinal chemistry letters.

[291]  Li Lin,et al.  Small Molecule c-jun-N-terminal Kinase (JNK) Inhibitors Protect Dopaminergic Neurons in a Model of Parkinson's Disease. , 2011, ACS chemical neuroscience.

[292]  Fanqi Qu,et al.  Bitriazolyl Acyclonucleosides with Antiviral Activity against Tobacco Mosaic Virus , 2008 .

[293]  I. Chaiken,et al.  Broad-Spectrum Anti-Human Immunodeficiency Virus (HIV) Potential of a Peptide HIV Type 1 Entry Inhibitor , 2007, Journal of Virology.

[294]  A. Tempone,et al.  Amphibian secretions for drug discovery studies: A search for new antiparasitic and antifungal compounds , 2007 .

[295]  G. Bifulco,et al.  Structure-based discovery of inhibitors of microsomal prostaglandin E2 synthase-1, 5-lipoxygenase and 5-lipoxygenase-activating protein: promising hits for the development of new anti-inflammatory agents. , 2011, Journal of medicinal chemistry.

[296]  A. Kozikowski,et al.  A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. , 2008, Journal of medicinal chemistry.

[297]  Nidhi Mishra,et al.  Synthesis of novel substituted 1,3-diaryl propenone derivatives and their antimalarial activity in vitro. , 2008, European journal of medicinal chemistry.

[298]  Ahmed Kamal,et al.  Synthesis of 1,2,3-triazole-linked pyrrolobenzodiazepine conjugates employing 'click' chemistry: DNA-binding affinity and anticancer activity. , 2008, Bioorganic & medicinal chemistry letters.

[299]  A. Shafiee,et al.  2-Hydroxyphenacyl azoles and related azolium derivatives as antifungal agents. , 2008, Bioorganic & medicinal chemistry letters.

[300]  A. Kojima,et al.  Synthesis and structure-activity relationship studies of highly potent novel oxazolidinone antibacterials. , 2008, Journal of medicinal chemistry.

[301]  J. McKerrow,et al.  A Cysteine Protease Inhibitor Protects Dogs from Cardiac Damage during Infection by Trypanosoma cruzi , 2005, Antimicrobial Agents and Chemotherapy.

[302]  A. Pupi,et al.  Click-chemistry-derived triazole ligands of arginine-glycine-aspartate (RGD) integrins with a broad capacity to inhibit adhesion of melanoma cells and both in vitro and in vivo angiogenesis. , 2010, Journal of medicinal chemistry.

[303]  Eun-Mi Kim,et al.  Synthesis of Tc-99m labeled 1,2,3-triazole-4-yl c-met binding peptide as a potential c-met receptor kinase positive tumor imaging agent. , 2010, Bioorganic & medicinal chemistry letters.