Highly functionalized 7-azaindoles as selective PPARγ modulators

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• 作者：Sheryl D. Debenham ; Audrey Chan ; Fiona WaiYu Lau ; Weiguo Liu ; Harold B. Wood ; Karen Lemme ; Lawrence Colwell ; Bahanu Habulihaz ; Taro E. Akiyama ; Monica Einstein ; Thomas W. Doebber ; Neelam Sharma ; Chaun
• 关键词：PPAR ; Azaindole ; Indole ; Selective PPAR modulator ; SPPARM
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：1 September 2008
• 年：2008
• 卷：18
• 期：17
• 页码：4798-4801
• 全文大小：173 K

文摘

A series of highly functionalized 3-aroyl and 3-phenoxy-2-methyl-7-azaindoles have been identified, which are potent selective PPARγ modulators (SPPARγMs). Addition of substituents at the 6-position of the 7-azaindoles improves in vitro potency and pharmacokinetics. 7-Azaindoles have significantly improved off-target profiles compared to the parent indole series.