Highly functionalized 7-azaindoles as selective PPAR gamma modulators

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4798-801. doi: 10.1016/j.bmcl.2008.07.103. Epub 2008 Jul 30.

Abstract

A series of highly functionalized 3-aroyl and 3-phenoxy-2-methyl-7-azaindoles have been identified, which are potent selective PPARgamma modulators (SPPARgammaMs). 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.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Humans
  • Indoles / chemistry*
  • Indoles / pharmacology*
  • Mice
  • PPAR gamma / agonists
  • PPAR gamma / metabolism*
  • Rats
  • Rats, Sprague-Dawley

Substances

  • 7-azaindole dimer
  • Indoles
  • PPAR gamma