Highly functionalized 7-azaindoles as selective PPARγ modulators

A series of highly functionalized 3-aroyl and 3-phenoxy-2-methyl-7-azaindoles have been identified, which are potent selective PPARγ modulators (SPPARγMs). The SAR around substitution at the 6-position of the azaindole as well as substitution of the N-benzyl moiety is reported. 7-Azaindoles have significantly improved off-target profiles compared to the parent indole series. 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.