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Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core

✍ Scribed by Dong-Ming Shen; Edward J. Brady; Mari R. Candelore; Qing Dallas-Yang; Victor D.-H. Ding; William P. Feeney; Guoquiang Jiang; Margaret E. McCann; Steve Mock; Sajjad A. Qureshi; Richard Saperstein; Xiaolan Shen; Xinchun Tong; Laurie M. Tota; Michael J. Wright; Xiaodong Yang; Song Zheng; Kevin T. Chapman; Bei B. Zhang; James R. Tata; Emma R. Parmee

Publisher: Elsevier Science
Year: 2011
Tongue: English
Weight: 461 KB
Volume: 21
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.11.074

No coin nor oath required. For personal study only.

✦ Synopsis

A novel class of 1,3,5-pyrazoles has been discovered as potent human glucagon receptor antagonists. Notably, compound 26 is orally bioavailable in several preclinical species and shows selectivity towards cardiac ion channels, other family B receptors such hGIP and hGLP1, and a large panel of enzymes and additional receptors. When dosed orally, compound 26 is efficacious in suppressing glucagon induced plasma glucose excursion in rhesus monkey and transgenic murine pharmacodynamic models at 1 and 10 mpk, respectively.

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