1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.

[1]  Gerhard Wolber,et al.  Arginase Structure and Inhibition: Catalytic Site Plasticity Reveals New Modulation Possibilities , 2017, Scientific Reports.

[2]  L. Cantley,et al.  α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH). , 2017, Journal of medicinal chemistry.

[3]  W. Gutheil,et al.  Cytoplasmic peptidoglycan intermediate levels in Staphylococcus aureus. , 2016, Biochimie.

[4]  C. Supuran,et al.  Interaction of carbonic anhydrase isozymes I, II, and IX with some pyridine and phenol hydrazinecarbothioamide derivatives. , 2015, Bioorganic & medicinal chemistry letters.

[5]  P. Paneth,et al.  Design, synthesis and biological evaluation of 4-benzoyl-1-dichlorobenzoylthiosemicarbazides as potent Gram-positive antibacterial agents , 2015, Journal of enzyme inhibition and medicinal chemistry.

[6]  A. Malm,et al.  Structure–activity Relationship Studies of Microbiologically Active Thiosemicarbazides Derived from Hydroxybenzoic Acid Hydrazides , 2015, Chemical biology & drug design.

[7]  M. Mostafa,et al.  Synthesis of novel binary and ternary complexes derived from 1-(2-hydroxy benzoyl)-4-phenylthiosemicarbazide (L(1)) and 2,2'-dipyridyl (L(2)) with Co(II), Cu(II) and Zn(II) salts. , 2015, Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy.

[8]  G. Sheldrick Crystal structure refinement with SHELXL , 2015, Acta crystallographica. Section C, Structural chemistry.

[9]  R. Powers,et al.  Metabolomics analysis identifies d-Alanine-d-Alanine ligase as the primary lethal target of d-Cycloserine in mycobacteria. , 2014, Journal of proteome research.

[10]  B. Villoutreix,et al.  Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group. , 2013, European journal of medicinal chemistry.

[11]  G. Prosser,et al.  Reinterpreting the Mechanism of Inhibition of Mycobacterium tuberculosisd-Alanine:d-Alanine Ligase by d-Cycloserine , 2013, Biochemistry.

[12]  G. Prosser,et al.  Kinetic mechanism and inhibition of Mycobacterium tuberculosis d‐alanine:d‐alanine ligase by the antibiotic d‐cycloserine , 2013, The FEBS Journal.

[13]  Stanislav Gobec,et al.  6-Arylpyrido[2,3-d]pyrimidines as Novel ATP-Competitive Inhibitors of Bacterial D-Alanine:D-Alanine Ligase , 2012, PloS one.

[14]  Janez Konc,et al.  Function of the D-alanine:D-alanine ligase lid loop: a molecular modeling and bioactivity study. , 2012, Journal of medicinal chemistry.

[15]  N. Strynadka,et al.  Structural perspective of peptidoglycan biosynthesis and assembly. , 2012, Annual review of biochemistry.

[16]  Jon Winter,et al.  Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation. , 2012, Journal of medicinal chemistry.

[17]  A. Plowright,et al.  Oxadiazoles in medicinal chemistry. , 2012, Journal of medicinal chemistry.

[18]  H. Schweizer,et al.  Characterization of d‐boroAla as a Novel Broad‐Spectrum Antibacterial Agent Targeting d‐Ala‐d‐Ala Ligase , 2011, Chemical biology & drug design.

[19]  Janez Konc,et al.  Ellipticines and 9-acridinylamines as inhibitors of D-alanine:D-alanine ligase. , 2011, Bioorganic & medicinal chemistry.

[20]  P. Paneth,et al.  Biological and docking studies of topoisomerase IV inhibition by thiosemicarbazides , 2011, Journal of molecular modeling.

[21]  A. Malm,et al.  Synthesis and antimicrobial activity of thiosemicarbazides, s-triazoles and their Mannich bases bearing 3-chlorophenyl moiety. , 2011, European journal of medicinal chemistry.

[22]  N. F. Thomas,et al.  Synthesis, Characterization and Antifungal Evaluation of 5-Substituted-4-Amino-1,2,4-Triazole-3-Thioesters , 2011, Molecules.

[23]  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.

[24]  P. Courvalin,et al.  Inducible expression eliminates the fitness cost of vancomycin resistance in enterococci , 2010, Proceedings of the National Academy of Sciences of the United States of America.

[25]  Nasim Hasan Rama,et al.  Identification of novel urease inhibitors by high-throughput virtual and in vitro screening. , 2010, ACS medicinal chemistry letters.

[26]  Françoise Van Bambeke,et al.  Structure-Based Design of Benzoxazoles as new Inhibitors for D-Alanyl - D-Alanine Ligase , 2009 .

[27]  J. Poupaert,et al.  DD-ligases as a potential target for antibiotics: past, present and future. , 2009, Current medicinal chemistry.

[28]  Samo Turk,et al.  Design and synthesis of new hydroxyethylamines as inhibitors of D-alanyl-D-lactate ligase (VanA) and D-alanyl-D-alanine ligase (DdlB). , 2009, Bioorganic & medicinal chemistry letters.

[29]  Stefan Wetzel,et al.  ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds. , 2009, Bioorganic & medicinal chemistry.

[30]  Janez Konc,et al.  Discovery of new inhibitors of D-alanine:D-alanine ligase by structure-based virtual screening. , 2008, Journal of medicinal chemistry.

[31]  Hualiang Jiang,et al.  D-Alanine:D-alanine ligase as a new target for the flavonoids quercetin and apigenin. , 2008, International journal of antimicrobial agents.

[32]  J. Hughes,et al.  Physiochemical drug properties associated with in vivo toxicological outcomes. , 2008, Bioorganic & medicinal chemistry letters.

[33]  J. Wouters,et al.  Disulfiram is an Inhibitor of Human Purified Monoacylglycerol Lipase, the Enzyme Regulating 2‐Arachidonoylglycerol Signaling , 2007, Chembiochem : a European journal of chemical biology.

[34]  I. Chopra,et al.  Diazenedicarboxamides as inhibitors of D-alanine-D-alanine ligase (Ddl). , 2007, Bioorganic & Medicinal Chemistry Letters.

[35]  K. Marotti,et al.  Allosteric inhibition of Staphylococcus aureus d-alanine:d-alanine ligase revealed by crystallographic studies , 2006, Proceedings of the National Academy of Sciences.

[36]  Seong-Hwan Rho,et al.  Crystal structure of the apo form of D‐alanine: D‐alanine ligase (Ddl) from Thermus caldophilus: A basis for the substrate‐induced conformational changes , 2006, Proteins.

[37]  M. Burkitt,et al.  Identification of a Two-Partner Secretion Locus of Enterotoxigenic Escherichia coli , 2006, Infection and Immunity.

[38]  L. Silver Does the cell wall of bacteria remain a viable source of targets for novel antibiotics? , 2006, Biochemical pharmacology.

[39]  C. Fishwick,et al.  A de novo designed inhibitor of D-Ala-D-Ala ligase from E. coli. , 2005, Angewandte Chemie.

[40]  Robert A Copeland,et al.  Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists. , 2005, Methods of biochemical analysis.

[41]  P. Courvalin,et al.  VanE-Type Vancomycin-Resistant Enterococcus faecalis Clinical Isolates from Australia , 2004, Antimicrobial Agents and Chemotherapy.

[42]  H. Brückner,et al.  Marfey’s reagent for chiral amino acid analysis: A review , 2004, Amino Acids.

[43]  B. Shoichet,et al.  A specific mechanism of nonspecific inhibition. , 2003, Journal of medicinal chemistry.

[44]  C. Chung,et al.  Effect of detergent on "promiscuous" inhibitors. , 2003, Journal of medicinal chemistry.

[45]  Atta-ur-Rahman,et al.  Synthesis and in vitro leishmanicidal activity of some hydrazides and their analogues. , 2003, Bioorganic & medicinal chemistry.

[46]  Stephen R. Johnson,et al.  Molecular properties that influence the oral bioavailability of drug candidates. , 2002, Journal of medicinal chemistry.

[47]  G. Gambetta,et al.  Genetic engineering of phytochrome biosynthesis in bacteria , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[48]  Mary Jane Ferraro,et al.  Linezolid resistance in a clinical isolate of Staphylococcus aureus , 2001, The Lancet.

[49]  S. David Synergic activity of D-cycloserine and beta-chloro-D-alanine against Mycobacterium tuberculosis. , 2001, The Journal of antimicrobial chemotherapy.

[50]  P. Selzer,et al.  Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties. , 2000, Journal of medicinal chemistry.

[51]  P. Courvalin,et al.  Vancomycin-Dependent Enterococcus faecalis Clinical Isolates and Revertant Mutants , 1999, Antimicrobial Agents and Chemotherapy.

[52]  C. Walsh,et al.  D-alanine:D-alanine ligase: phosphonate and phosphinate intermediates with wild type and the Y216F mutant. , 1997, Biochemistry.

[53]  M. Arthur,et al.  Glycopeptide resistance in enterococci. , 1996, Trends in microbiology.

[54]  P. Tulkens,et al.  Effect of recombinant human gamma interferon on intracellular activities of antibiotics against Listeria monocytogenes in the human macrophage cell line THP-1 , 1996, Antimicrobial agents and chemotherapy.

[55]  D. Belin,et al.  Tight regulation, modulation, and high-level expression by vectors containing the arabinose PBAD promoter , 1995, Journal of bacteriology.

[56]  C. Walsh,et al.  Active site mapping of Escherichia coli D-Ala-D-Ala ligase by structure-based mutagenesis. , 1995, Biochemistry.

[57]  C. Walsh,et al.  Vancomycin resistance: structure of D-alanine:D-alanine ligase at 2.3 A resolution. , 1994, Science.

[58]  B. Spratt Resistance to antibiotics mediated by target alterations. , 1994, Science.

[59]  W. Yew,et al.  Adverse neurological reactions in patients with multidrug-resistant pulmonary tuberculosis after coadministration of cycloserine and ofloxacin. , 1993, Clinical infectious diseases : an official publication of the Infectious Diseases Society of America.

[60]  C. Walsh,et al.  D-Alanyl-D-alanine ligases and the molecular mechanism of vancomycin resistance , 1992 .

[61]  H. Brückner,et al.  High-performance liquid chromatographic separation of dl-amino acids derivatized with chiral variants of Sanger's reagent☆ , 1991 .

[62]  C. Walsh,et al.  Existence of two D-alanine:D-alanine ligases in Escherichia coli: cloning and sequencing of the ddlA gene and purification and characterization of the DdlA and DdlB enzymes. , 1991, Biochemistry.

[63]  C. Le Bouguénec,et al.  Presence of chromosomal elements resembling the composite structure Tn3701 in streptococci , 1990, Journal of bacteriology.

[64]  W. Greenlee,et al.  (3-Amino-2-oxoalkyl)phosphonic acids and their analogues as novel inhibitors of D-alanine:D-alanine ligase. , 1989, Journal of medicinal chemistry.

[65]  C. Walsh,et al.  (1-Aminoethyl)boronic acid: a novel inhibitor for Bacillus stearothermophilus alanine racemase and Salmonella typhimurium D-alanine:D-alanine ligase (ADP-forming). , 1989, Biochemistry.

[66]  J. Springer,et al.  Phosphinic acid inhibitors of D-alanyl-D-alanine ligase. , 1988, Journal of medicinal chemistry.

[67]  C. Walsh,et al.  ATP-dependent inactivation and slow binding inhibition of Salmonella typhimurium D-alanine:D-alanine ligase (ADP) by (aminoalkyl)phosphinate and aminophosphonate analogues of D-alanine. , 1988, Biochemistry.

[68]  O. Takikawa,et al.  Mechanism of interferon-gamma action. Characterization of indoleamine 2,3-dioxygenase in cultured human cells induced by interferon-gamma and evaluation of the enzyme-mediated tryptophan degradation in its anticellular activity. , 1988, The Journal of biological chemistry.

[69]  D. Carniato,et al.  (1-Amino-2-propenyl) phosphonic acid, an inhibitor of alanine racemase and D-alanine:D-alanine ligase. , 1986, Journal of medicinal chemistry.

[70]  Shigeru Tsuchiya,et al.  Establishment and characterization of a human acute monocytic leukemia cell line (THP‐1) , 1980, International journal of cancer.

[71]  P. A. Lanzetta,et al.  An improved assay for nanomole amounts of inorganic phosphate. , 1979, Analytical biochemistry.

[72]  A. Jacob,et al.  Conjugal Transfer of Plasmid-Borne Multiple Antibiotic Resistance in Streptococcus faecalis var. zymogenes , 1974, Journal of bacteriology.

[73]  U. K. Laemmli,et al.  Cleavage of Structural Proteins during the Assembly of the Head of Bacteriophage T4 , 1970, Nature.

[74]  F C NEUHAUS,et al.  THE ENZYMATIC SYNTHESIS OF D-ALANYL-D-ALANINE. 3. ON THE INHIBITION OF D-ALANYL-D-ALANINE SYNTHETASE BY THE ANTIBIOTIC D-CYCLOSERINE. , 1964, Biochemistry.

[75]  F. Neuhaus The enzymatic synthesis of D-alanyl-D-alanine. II. Kinetic studies on D-alanyl-D-alanine synthetase. , 1962, The Journal of biological chemistry.

[76]  W. Gutheil,et al.  A liquid chromatography-tandem mass spectrometry assay for Marfey's derivatives of L-Ala, D-Ala, and D-Ala-D-Ala: application to the in vivo confirmation of alanine racemase as the target of cycloserine in Escherichia coli. , 2010, Analytical biochemistry.

[77]  P. C. Jalihal,et al.  Synthesis and antimicrobial activity of some new 2,5 disubstituted 1,3,4-thiadiazoles. , 2009 .

[78]  W. Strober Trypan blue exclusion test of cell viability. , 2001, Current protocols in immunology.

[79]  P. Bartlett,et al.  Synthesis and evaluation of inhibitors of bacterial D-alanine:D-alanine ligases. , 1996, Chemistry & biology.

[80]  W. Hammes,et al.  Inhibition of cell wall biosynthesis by analogues of alanine , 1981 .

[81]  E. Hoggarth,et al.  327. Compounds related to thiosemicarbazide. Part VII. Benzylthiosemicarbazides , 1949 .