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Highly functionalized 7-azaindoles as selective PPAR gamma modulators |
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| Authors: | Debenham Sheryl D Chan Audrey Lau Fiona Waiyu Liu Weiguo Wood Harold B Lemme Karen Colwell Lawrence Habulihaz Bahanu Akiyama Taro E Einstein Monica Doebber Thomas W Sharma Neelam Wang Chaunlin F Wu Margaret Berger Joel P Meinke Peter T |
| Institution: | aMerck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA |
| Abstract: | 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. |
| Keywords: | PPAR Azaindole Indole Selective PPAR modulator SPPARM |
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