Publications by authors named "Joseph Pontillo"

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Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics.
Joseph Pontillo, Dongpei Wu, Brett Ching, Sarah Hudson, Marc J Genicot

Bioorg Med Chem Lett· December 2008

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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.
Chen Chen, Dongpei Wu, Zhiqiang Guo, Qiu Xie, Greg J Reinhart, Joseph Pontillo

J Med Chem· December 2008

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Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
Dongpei Wu, Joseph Pontillo, Brett Ching, Sarah Hudson, Yinghong Gao

Bioorg Med Chem Lett· July 2008

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Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.
Chen Chen, Yongsheng Chen, Joseph Pontillo, Zhiqiang Guo, Charles Q Huang

Bioorg Med Chem Lett· June 2008

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Studies on the structure-activity relationship of the basic amine of phenylpiperazines as melanocortin-4 receptor antagonists.
Joe A Tran, Melissa Arellano, Beth A Fleck, Joseph Pontillo, Dragan Marinkovic

Med Chem· January 2008

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Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Joe A Tran, Fabio C Tucci, Wanlong Jiang, Dragan Marinkovic, Caroline W Chen, Joseph Pontillo

Bioorg Med Chem· August 2007

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Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor.
Wanlong Jiang, Fabio C Tucci, Caroline W Chen, Melissa Arellano, Joe A Tran, Joseph Pontillo

Bioorg Med Chem Lett· September 2006

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Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2.
Sarah Hudson, Mehrak Kiankarimi, Martin W Rowbottom, Troy D Vickers, Dongpei Wu, Joseph Pontillo

Bioorg Med Chem Lett· September 2006

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Propionylpiperazines as human melanocortin-4 receptor ligands.
Caroline W Chen, Joe A Tran, Wanlong Jiang, Fabio C Tucci, Melissa Arellano, Joseph Pontillo

Bioorg Med Chem Lett· September 2006

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Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists.
Brian Dyck, Liren Zhao, Junko Tamiya, Joseph Pontillo, Sarah Hudson

Bioorg Med Chem Lett· August 2006

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Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor.
Joe A Tran, Joseph Pontillo, Beth A Fleck, Dragan Marinkovic, Melissa Arellano

Bioorg Med Chem Lett· July 2006

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Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor.
Joseph Pontillo, Joe A Tran, Nicole S White, Melissa Arellano, Beth A Fleck

Bioorg Med Chem Lett· December 2005

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Synthesis of aryl-1,2,4-triazine-3,5-diones as antagonists of the gonadotropin-releasing hormone receptor.
Joseph Pontillo, Zhiqiang Guo, Dongpei Wu, R Scott Struthers, Chen Chen

Bioorg Med Chem Lett· October 2005

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Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines.
Fabio C Tucci, Nicole S White, Stacy Markison, Margaret Joppa, Joe A Tran, Joseph Pontillo

Bioorg Med Chem Lett· October 2005

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Optimization of piperazinebenzylamines with a N-(1-methoxy-2-propyl) side chain as potent and selective antagonists of the human melanocortin-4 receptor.
Joseph Pontillo, Dragan Marinkovic, Joe A Tran, Melissa Arellano, Beth A Fleck

Bioorg Med Chem Lett· October 2005

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Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.
Joseph A Tran, Joseph Pontillo, Melissa Arellano, Beth A Fleck, Fabio C Tucci

Bioorg Med Chem Lett· July 2005

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Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers.
Zhiqiang Guo, Yongsheng Chen, Charles Q Huang, Timothy D Gross, Joseph Pontillo

Bioorg Med Chem Lett· May 2005

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A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice.
Joseph Pontillo, Joseph A Tran, Stacy Markison, Margaret Joppa, Beth A Fleck

Bioorg Med Chem Lett· May 2005

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Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists.
Joseph Pontillo, Chen Chen

Bioorg Med Chem Lett· March 2005

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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.
Zhiqiang Guo, Dongpei Wu, Yun-Fei Zhu, Fabio C Tucci, Joseph Pontillo

Bioorg Med Chem Lett· February 2005

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Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines.
Joe A Tran, Joseph Pontillo, Melissa Arellano, Nicole S White, Beth A Fleck

Bioorg Med Chem Lett· February 2005

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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.
Chen Chen, Joseph Pontillo, Beth A Fleck, Yinghong Gao, Jenny Wen

J Med Chem· December 2004

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Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor.
Joseph Pontillo, Joseph A Tran, Beth A Fleck, Dragan Marinkovic, Melissa Arellano

Bioorg Med Chem Lett· November 2004

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Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.
Joseph Pontillo, Joseph A Tran, Melissa Arellano, Beth A Fleck, Rajesh Huntley

Bioorg Med Chem Lett· September 2004

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Synthetic approach to analogues of the original structure of sclerophytin A.
Michael E Jung, Joseph Pontillo

J Org Chem· September 2002

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