title: Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
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.
authors.affiliation: Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
authors.forename: Sheryl D
authors.initials: SD
authors.lastname: Debenham
authors.forename: Audrey
authors.initials: A
authors.lastname: Chan
authors.forename: Fiona Waiyu
authors.initials: FW
authors.lastname: Lau
authors.forename: Weiguo
authors.initials: W
authors.lastname: Liu
authors.forename: Harold B
authors.initials: HB
authors.lastname: Wood
authors.forename: Karen
authors.initials: K
authors.lastname: Lemme
authors.forename: Lawrence
authors.initials: L
authors.lastname: Colwell
authors.forename: Bahanu
authors.initials: B
authors.lastname: Habulihaz
authors.forename: Taro E
authors.initials: TE
authors.lastname: Akiyama
authors.forename: Monica
authors.initials: M
authors.lastname: Einstein
authors.forename: Thomas W
authors.initials: TW
authors.lastname: Doebber
authors.forename: Neelam
authors.initials: N
authors.lastname: Sharma
authors.forename: Chaunlin F
authors.initials: CF
authors.lastname: Wang
authors.forename: Margaret
authors.initials: M
authors.lastname: Wu
authors.forename: Joel P
authors.initials: JP
authors.lastname: Berger
authors.forename: Peter T
authors.initials: PT
authors.lastname: Meinke
mesh_terms: D000818:Animals; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D051379:Mice; D047495:PPAR gamma / Q000819:agonists / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: C023422:7-azaindole dimer; D007211:Indoles; D047495:PPAR gamma