Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
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.
Debenham
Sheryl D
SD
Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
Chan
Audrey
A
Lau
Fiona Waiyu
FW
Liu
Weiguo
W
Wood
Harold B
HB
Lemme
Karen
K
Colwell
Lawrence
L
Habulihaz
Bahanu
B
Akiyama
Taro E
TE
Einstein
Monica
M
Doebber
Thomas W
TW
Sharma
Neelam
N
Wang
Chaunlin F
CF
Wu
Margaret
M
Berger
Joel P
JP
Meinke
Peter T
PT
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
C023422:7-azaindole dimer; D007211:Indoles; D047495:PPAR gamma