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Basic Information

ID: ALA1641377

Journal: Bioorg Med Chem Lett

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

Authors: Shen DM, Brady EJ, Candelore MR, Dallas-Yang Q, Ding VD, Feeney WP, Jiang G, McCann ME, Mock S, Qureshi SA, Saperstein R, Shen X, Tong X, Tota LM, Wright MJ, Yang X, Zheng S, Chapman KT, Zhang BB, Tata JR, Parmee ER.

Abstract: 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.

CiteXplore: 21147532

DOI: 10.1016/j.bmcl.2010.11.074