F. Tucci

发表

Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists.

Zhiqian Guo, Chen Chen, S. K. Sullivan, 2005, Bioorganic & medicinal chemistry letters.

Influence of pKa on the biotransformation of indene H1-antihistamines by CYP2D6.

G. Beaton, S. Malany, P. Crowe, 2011, Bioorganic & medicinal chemistry letters.

Systemic TAK-242 prevents intrathecal LPS evoked hyperalgesia in male, but not female mice and prevents delayed allodynia following intraplantar formalin in both male and female mice: The role of TLR4 in the evolution of a persistent pain state

R. Isseroff, T. Yaksh, M. Corr, 2016, Brain, Behavior, and Immunity.

Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.

M. Bradbury, F. Jovic, G. Beaton, 2009, Journal of medicinal chemistry.

Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.

Zhiqian Guo, Chen Chen, Martin W Rowbottom, 2008, Bioorganic & medicinal chemistry letters.

Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.

S. Hoare, Beth A. Fleck, Joe A. Tran, 2008, Bioorganic & medicinal chemistry.

Nanoscale Container Structures and Their Host – Guest Properties

A. Renslo, J. Rebek, D. Rudkevich, 2000 .

Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5.

Zhiqian Guo, Chen Chen, S. K. Sullivan, 2004, Bioorganic & medicinal chemistry letters.

Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists.

Zhiqian Guo, Q. Xie, Chen Chen, 2004, Bioorganic & medicinal chemistry letters.

Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.

S. Hoare, Beth A. Fleck, Joe A. Tran, 2007, Bioorganic & medicinal chemistry letters.

A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists.

Zhiqian Guo, Chen Chen, J. Saunders, 2002, Bioorganic & medicinal chemistry letters.

An efficient preparation of functionalized Z-vinylcuprates from terminal acetylenes and their reactions with epoxides

J. Marino, J. Comasseto, F. Tucci, 1993 .

Oxazolium-derived azomethine ylides. External oxazole activation and internal dipole trapping in the synthesis of an aziridinomitosene.

E. Vedejs, D. W. Piotrowski, F. Tucci, 2000, The Journal of organic chemistry.

Enantiocontrolled Synthesis of (1S,2S)-6-Desmethyl-(methylaziridino)mitosene

E. Vedejs, A. Klapars, F. Tucci, 2000 .

Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines.

Beth A. Fleck, M. Joppa, B. Dyck, 2005, Bioorganic & medicinal chemistry letters.

Oxazolium-derived azomethine ylides. External oxazole activation and internal dipole trapping in the synthesis of an aziridinomitosene.

E. Vedejs, D. W. Piotrowski, D. Piotrowski, 2000, The Journal of organic chemistry.

Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.

Zhiqian Guo, Chen Chen, J. Saunders, 2008, Journal of medicinal chemistry.

5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.

Zhiqian Guo, Chen Chen, Yun-fei Zhu, 2008, Bioorganic & medicinal chemistry letters.

Stereocontrolled synthesis of (-)-macrolactin A.

J. Marino, D. Holub, J. Comasseto, 2002, Journal of the American Chemical Society.

Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands.

Beth A. Fleck, Joe A. Tran, A. Foster, 2008, Bioorganic & medicinal chemistry letters.

Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor.

S. Hoare, Beth A. Fleck, Joe A. Tran, 2007, Bioorganic & medicinal chemistry letters.

An Efficient Preparation of Functionalized Z‐Vinylcuprates from Terminal Acetylenes and Their Reactions with Epoxides.

J. Marino, J. Comasseto, F. Tucci, 1994 .

Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers.

Zhiqian Guo, Chen Chen, J. Saunders, 2005, Bioorganic & medicinal chemistry letters.

Synthesis and structure-activity relationships of 1-arylmethyl-5-aryl-6-methyluracils as potent gonadotropin-releasing hormone receptor antagonists.

Zhiqian Guo, Chen Chen, Yinghong Gao, 2004, Journal of medicinal chemistry.

Synthesis and structure-activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor.

Zhiqian Guo, Chen Chen, J. Saunders, 2003, Bioorganic & medicinal chemistry letters.

Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists.

Zhiqian Guo, Chen Chen, Yinghong Gao, 2003, Bioorganic & medicinal chemistry letters.

Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists.

Zhiqian Guo, Chen Chen, Yinghong Gao, 2003, Journal of medicinal chemistry.

Tellurium in Organic Synthesis. Preparation of Z-Vinylic Cuprates from Z-Vinylic Tellurides and Their Reaction with Enones and Epoxides

A. Chieffi, J. Marino, J. Comasseto, 1996 .

Higher order vinyl cyanocuprates from vinylic tellurides

A. Chieffi, J. Comasseto, F. Tucci, 1992 .

Atropisomeric property of 1-(2,6-difluorobenzyl)-3-[(2R)-amino-2-phenethyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyluracil.

N. Ling, Zhiqian Guo, M. Mesleh, 2005, Chirality.

A self-assembled cylindrical capsule: new supramolecular phenomena through encapsulation.

J. Rebek, D. Rudkevich, T. Heinz, 2000, Chemistry.

Synthesis and Assembly of Self-Complementary Cavitands

A. Renslo, J. Rebek, F. Tucci, 2000 .

Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.

M. Bradbury, G. Beaton, Jinghua Yu, 2010, Bioorganic & medicinal chemistry letters.

Self-Folding Cavitands of Nanoscale Dimensions

J. Rebek, U. Lücking, F. Tucci, 2000 .

Stereochemical Relationships between Encapsulated Molecules

J. Rebek, F. Tucci, and Dmitry M. Rudkevich, 1999 .

4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist--design, synthesis, and characterization.

Beth A. Fleck, Joe A. Tran, A. Foster, 2004, Journal of medicinal chemistry.

Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.

Zhiqian Guo, Chen Chen, Yinghong Gao, 2003, Journal of medicinal chemistry.

3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.

N. Ling, Zhiqian Guo, Xin-jun Liu, 2005, Journal of medicinal chemistry.

Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.

Beth A. Fleck, Joe A. Tran, A. Foster, 2004, Bioorganic & medicinal chemistry letters.

90 Efficacy of a Novel Small Molecule RORgt Inverse Agonist in Mouse DSS and TNBS Models of Inflammatory Bowel Disease

G. Alton, L. Fitzpatrick, Jeffrey S. Small, 2015 .

Therapeutic efficacy of α7 ligands after acute ischaemic stroke is linked to conductive states of α7 nicotinic ACh receptors

G. Beaton, Victor V Uteshev, W. Kem, 2021, British journal of pharmacology.

Novel benzothiophene H1-antihistamines for the treatment of insomnia.

Siobhan Malany, Bin-Feng Li, M. Bradbury, 2010, Bioorganic & medicinal chemistry letters.

A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists.

Zhiqian Guo, Chen Chen, J. Saunders, 2005, Bioorganic & medicinal chemistry letters.

Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor.

Beth A. Fleck, Joe A. Tran, A. Foster, 2006, Bioorganic & medicinal chemistry letters.

Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands.

Beth A. Fleck, Joe A. Tran, Chen Chen, 2008, Bioorganic & medicinal chemistry letters.

Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor.

Beth A. Fleck, Joe A. Tran, Chen Chen, 2007, Bioorganic & medicinal chemistry letters.

Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor.

Beth A. Fleck, Joe A. Tran, Beth A Fleck, 2007, Bioorganic & medicinal chemistry letters.

Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor.

S. Hoare, Beth A. Fleck, Joe A. Tran, 2008, Bioorganic & medicinal chemistry letters.

Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor.

Beth A. Fleck, Joe A. Tran, A. Foster, 2005, Bioorganic & medicinal chemistry letters.

Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.

Beth A. Fleck, Joe A. Tran, A. Foster, 2005, Bioorganic & medicinal chemistry letters.

Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines.

Beth A. Fleck, Joe A. Tran, A. Foster, 2005, Bioorganic & medicinal chemistry letters.

Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor.

Beth A. Fleck, Joe A. Tran, A. Foster, 2004, Bioorganic & medicinal chemistry letters.

Optimization of piperazinebenzylamines with a N-(1-methoxy-2-propyl) side chain as potent and selective antagonists of the human melanocortin-4 receptor.

Beth A. Fleck, Joe A. Tran, A. Foster, 2005, Bioorganic & medicinal chemistry letters.

A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice.

S. Hoare, Beth A. Fleck, M. Joppa, 2005, Bioorganic & medicinal chemistry letters.

Ligands de recepteurs de la melanocortine, compositions et procedes associes

Joe A. Tran, Wanlong Jiang, F. Tucci, 2004 .

Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor.

Beth A. Fleck, Joe A. Tran, A. Foster, 2006, Bioorganic & medicinal chemistry letters.

Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.

S. Hoare, Beth A. Fleck, M. Joppa, 2007, Journal of medicinal chemistry.

Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.

S. Hoare, Beth A. Fleck, Joe A. Tran, 2007, Journal of medicinal chemistry.

Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H₁-antihistamines for insomnia.

Joe A. Tran, G. Beaton, Jinghua Yu, 2012, Bioorganic & medicinal chemistry letters.

Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.

M. Bradbury, F. Jovic, G. Beaton, 2009, Journal of medicinal chemistry.

Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands.

Beth A. Fleck, Joe A. Tran, Chen Chen, 2008, Bioorganic & medicinal chemistry letters.

Practical asymmetric synthesis of alpha-branched 2-piperazinylbenzylamines by 1,2-additions of organometallic reagents to N-tert-butanesulfinyl imines.

C. Chen, Joe A. Tran, Wanlong Jiang, 2005, The Journal of organic chemistry.

A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists.

Zhiqian Guo, K. Wilcoxen, Chen Chen, 2002, Bioorganic & medicinal chemistry letters.