Discovery of a series of imidazo [4, 5-b] pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ

A Casimiro-Garcia, GF Filzen, D Flynn…

Index: Casimiro-Garcia, Agustin; Filzen, Gary F.; Flynn, Declan; Bigge, Christopher F.; Chen, Jing; Davis, Jo Ann; Dudley, Danette A.; Edmunds, Jeremy J.; Esmaeil, Nadia; Geyer, Andrew; Heemstra, Ronald J.; Jalaie, Mehran; Ohren, Jeffrey F.; Ostroski, Robert; Ellis, Teresa; Schaum, Robert P.; Stoner, Chad Journal of Medicinal Chemistry, 2011 , vol. 54, # 12 p. 4219 - 4233

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Citation Number: 31

Abstract

Mining of an in-house collection of angiotensin II type 1 receptor antagonists to identify compounds with activity at the peroxisome proliferator-activated receptor-γ (PPARγ) revealed a new series of imidazo [4, 5-b] pyridines 2 possessing activity at these two receptors. Early availability of the crystal structure of the lead compound 2a bound to the ligand binding domain of human PPARγ confirmed the mode of interaction of this scaffold ...