Benzimidazolones: A new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators

…, Y Li, TE Akiyama, G Castriota, M Einstein…

Index: Liu, Weiguo; Lau, Fiona; Liu, Kun; Wood, Harold B.; Zhou, Gaochao; Chen, Yuli; Li, Ying; Akiyama, Taro E.; Castriota, Gino; Einstein, Monica; Wang, Chualin; McCann, Margaret E.; Doebber, Thomas W.; Wu, Margaret; Chang, Ching H.; McNamara, Lesley; McKeever, Brian; Mosley, Ralph T.; Berger, Joel P.; Meinke, Peter T. Journal of Medicinal Chemistry, 2011 , vol. 54, # 24 p. 8541 - 8554

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Citation Number: 19

Abstract

A series of benzimidazolone carboxylic acids and oxazolidinediones were designed and synthesized in search of selective PPARγ modulators (SPPARγMs) as potential therapeutic agents for the treatment of type II diabetes mellitus (T2DM) with improved safety profiles relative to rosiglitazone and pioglitazone, the currently marketed PPARγ full agonist drugs. Structure–activity relationships of these potent and highly selective SPPARγMs were ...