Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Melissa Arellano"'
Autor:
Lan Zhang, Hanghui Liu, Brett Weylan Ching, Guy Servant, Tanya Ditschun, Andrew Patron, Thomas Brady, Mark C. Williams, Melissa Arellano, Vincent Darmohusodo, Michael Saganich, Qing Chen, Timothy Davis, Catherine Tachdjian, Donald S. Karanewsky, Joseph R. Fotsing
Publikováno v:
Journal of medicinal chemistry. 63(9)
In humans, bitter taste is mediated by 25 TAS2Rs. Many compounds, including certain active pharmaceutical ingredients, excipients, and nutraceuticals, impart their bitter taste (or in part) through TAS2R8 activation. However, effective TAS2R8 blocker
Autor:
Wilna J. Moree, Paul D. Crowe, Jianyun Wen, Siobhan Malany, Fabio C. Tucci, Sam R. J. Hoare, Melissa Arellano, Graham Beaton, Bin-Feng Li, Jinghua Yu, Joe A. Tran, Satheesh B. Ravula, Robert E. Petroski, Ajay Madan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:421-426
The structure–activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles, 2-morpholine and 2-thiomorpholin-2-yl-1H-benzimidazoles are described. In the lead optimization process, the pKa and/or log P of benzimidazole analogs were reduced either
Autor:
Joe A. Tran, Melissa Arellano, Stacy Markison, John Saunders, Ajay Madan, Dragan Marinkovic, Chen Chen, Sam R. J. Hoare, Alan C. Foster, Beth A. Fleck, Jenny Wen, Fabio C. Tucci, Caroline W. Chen, Wanlong Jiang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:129-136
A series of trans-4-phenylpyrrolidine-3-carboxamides were synthesized and characterized as potent ligands of the human melanocortin-4 receptor. Interestingly, a pair of diastereoisomers 13b displayed potent functional agonist and antagonist activity,
Autor:
Stacy Markison, Melissa Arellano, Joe A. Tran, Haig Bozigian, Caroline W. Chen, Wanlong Jiang, John Saunders, Fabio C. Tucci, Beth A. Fleck, Ajay Madan, Daniel Marks, Ta Kung Chen, Chen Chen, Yang Sai, John Harman, Dragan Marinkovic, Alan C. Foster, Jenny Wen, Sam R. J. Hoare
Publikováno v:
Journal of Medicinal Chemistry. 50:6356-6366
Benzylamine and pyridinemethylamine derivatives were synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor (MC4R). These compounds were also profiled in rodents for their pharmacokinetic properties. Two comp
Autor:
Michael Johns, Beth A. Fleck, Ajay Madan, Dragan Marinkovic, Margaret Joppa, Chen Chen, Stacy Markison, Wanlong Jiang, Melissa Arellano, Alan C. Foster, Joe A. Tran, Fabio C. Tucci, Takung Chen, Jenny Wen, Yang Sai, Sam R. J. Hoare, Caroline W. Chen, John Saunders
Publikováno v:
Journal of Medicinal Chemistry. 50:5249-5252
A potent and selective antagonist of the melanocortin-4 receptor, 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-6-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine (10d), was identified from a series piperazinebenzylami
Autor:
Alan C. Foster, Wanlong Jiang, John Saunders, Beth A. Fleck, Jenny Wen, Dragan Marinkovic, Stacy Markison, Michael Johns, Chen Chen, Sam R. J. Hoare, Melissa Arellano, Joe A. Tran, Caroline W. Chen, Fabio C. Tucci
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5610-5613
A series of pyrrolidinones derived from phenylalaninepiperazines were synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor. In addition to their high binding affinities, these compounds displayed high funct
Autor:
Joe A. Tran, Nicole S. White, Jenny Wen, Joseph Pontillo, John Saunders, Caroline W. Chen, Dragan Marinkovic, Ajay Madan, Chen Chen, Alan C. Foster, Beth A. Fleck, Fabio C. Tucci, Wanlong Jiang, Melissa Arellano
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4800-4803
A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain penetration i
Autor:
Dragan Marinkovic, Alan C. Foster, Nicole S. White, Melissa Arellano, John Saunders, Jenny Wen, Joe A. Tran, Chen Chen, Joseph Pontillo, Beth A. Fleck, Wanlong Jiang, Fabio C. Tucci
Publikováno v:
Letters in Drug Design & Discovery. 3:311-315
Autor:
Marion Lanier, Joseph Pontillo, Melissa Arellano, Wanlong Jiang, Chen Chen, Dragan Marinkovic, John Saunders, Alan C. Foster, Fabio C. Tucci, Caroline W. Chen, Beth A. Fleck, Joe A. Tran
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3693-3696
A series of 2-pyridinylpiperazines derived from β-Ala-(2,4-Cl)Phe dipeptide was synthesized for the study of their SARs and possible interactions with the MC4 receptor. Compounds such as 11k (Ki = 6.5 nM) possessed high potency.
Autor:
Beth A. Fleck, Joseph Pontillo, Nicole S. White, Fabio C. Tucci, John Saunders, Joe A. Tran, Dragan Marinkovic, Alan C. Foster, Melissa Arellano, Chen Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5237-5240
Synthesis and structure-activity relationship studies of a series of cyclohexylpiperazines bearing an amide side chain as ligands of the MC4 receptor are discussed. Compounds such as 11i from this series are potent agonists (EC(50)=33nM, IA=96%).