Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.
The discovery and optimization of a series of potent PPARdelta full agonists with partial agonistic activity against PPARgamma is described.
Connors
Richard V
RV
Department of Chemistry, Amgen, 1120 Veterans Blvd., South San Francisco, CA 94080, USA. rconnors@amgen.com
Wang
Zhulun
Z
Harrison
Martin
M
Zhang
Alex
A
Wanska
Malgorzata
M
Hiscock
Steve
S
Fox
Brian
B
Dore
Michael
M
Labelle
Marc
M
Sudom
Athena
A
Johnstone
Sheree
S
Liu
Jinsong
J
Walker
Nigel P C
NP
Chai
Anne
A
Siegler
Karen
K
Li
Yang
Y
Coward
Peter
P
D000818:Animals; D003198:Computer Simulation; D018360:Crystallography, X-Ray; D047494:PPAR delta / Q000819:agonists* / Q000378:metabolism; D047495:PPAR gamma / Q000819:agonists* / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D047494:PPAR delta; D047495:PPAR gamma; D013844:Thiazoles