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

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

文献索引: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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被引用次数: 19

摘要

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 ...