Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists

G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes since it was shown clinically to promote glucose-stimulated insulin secretion. Herein, we report our efforts to develop highly selective and potent GPR40 agonists with a dual mechanism of action, prom...

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Published in:	Journal of medicinal chemistry 2018-02, Vol.61 (3), p.681-694
Main Authors:	Shi, Jun, Gu, Zhengxiang, Jurica, Elizabeth Anne, Wu, Ximao, Haque, Lauren E, Williams, Kristin N, Hernandez, Andres S, Hong, Zhenqiu, Gao, Qi, Dabros, Marta, Davulcu, Akin H, Mathur, Arvind, Rampulla, Richard A, Gupta, Arun Kumar, Jayaram, Ramya, Apedo, Atsu, Moore, Douglas B, Liu, Heng, Kunselman, Lori K, Brady, Edward J, Wilkes, Jason J, Zinker, Bradley A, Cai, Hong, Shu, Yue-Zhong, Sun, Qin, Dierks, Elizabeth A, Foster, Kimberly A, Xu, Carrie, Wang, Tao, Panemangalore, Reshma, Cvijic, Mary Ellen, Xie, Chunshan, Cao, Gary G, Zhou, Min, Krupinski, John, Whaley, Jean M, Robl, Jeffrey A, Ewing, William R, Ellsworth, Bruce Alan
Format:	Article
Language:	English
Subjects:	Administration, Oral Animals Biological Availability Drug Discovery Humans Male Mice Models, Molecular Molecular Conformation Pyrazoles - administration & dosage Pyrazoles - chemistry Pyrazoles - pharmacokinetics Pyrazoles - pharmacology Pyrrolidines - chemistry Receptors, G-Protein-Coupled - agonists
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