Title of article
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor
Author/Authors
Joseph L. Duffy، نويسنده , , Brian A. Kirk، نويسنده , , Zenon Konteatis، نويسنده , , Elizabeth L. Campbell، نويسنده , , Rui Liang، نويسنده , , Edward J. Brady، نويسنده , , Mari Rios Candelore، نويسنده , , Victor D.H. Ding، نويسنده , , Guoqiang Jiang، نويسنده , , Xiaoqing Frank Liu، نويسنده , , Sajjad A. Qureshi، نويسنده , , Richard Saperstein، نويسنده , , Deborah Szalkowski، نويسنده , , Sharon Tong، نويسنده , , Lauri M. Tota، نويسنده , , Dan Xie and Guoliang Ji ، نويسنده , , Xiaoyan Ye and Xiaodong Yang، نويسنده , , Peter Zafian، نويسنده , , Song Zheng، نويسنده , , Kevin T. Chapman، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
1401
To page
1405
Abstract
A novel class of antagonists of the human glucagon receptor (hGCGR) has been discovered. Systematic modification of the lead compound identified substituents that were essential for activity and those that were amenable to further optimization. This SAR exploration resulted in the synthesis of 13, which exhibited good potency as an hGCGR functional antagonist (IC50 = 34 nM) and moderate bioavailability (36% in mice).
Keywords
Gewald , glucagon , Diabetes , Thiophene
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795405
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