Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
作者信息
Duffy Joseph L, Kirk Brian A, Konteatis Zenon, Campbell Elizabeth L, Liang Rui, Brady Edward J, Candelore Mari Rios, Ding Victor D H, Jiang Guoqiang, Liu Frank, Qureshi Sajjad A, Saperstein Richard, Szalkowski Deborah, Tong Sharon, Tota Lauri M, Xie Dan, Yang Xiaodong, Zafian Peter, Zheng Song, Chapman Kevin T, Zhang Bei B, Tata James R
机构信息
Department of Basic Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2005 Mar 1;15(5):1401-5. doi: 10.1016/j.bmcl.2005.01.003.
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).
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