Discovery and SAR of para-alkylthiophenoxyacetic acids as potent and selective PPARdelta agonists.
Synthesis and SAR of para-alkylthiophenoxyacetic acids is described. Achiral compounds 30, 31 and 32 were identified as potent and selective PPARdelta agonists.
Zhang
Rui
R
Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, 8 Clarke Drive, Cranbury, NJ 08512, USA. rzhang4@prdus.jnj.com
Deangelis
Alan
A
Wang
Aihua
A
Sieber-McMaster
Ellen
E
Li
Xun
X
Russell
Ronald
R
Pelton
Patricia
P
Xu
Jun
J
Zhu
Peifang
P
Zhou
Lubing
L
Demarest
Keith
K
Murray
William V
WV
Kuo
Gee-Hong
GH
D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D055808:Drug Discovery; D004353:Drug Evaluation, Preclinical; D006016:Glycolates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D047494:PPAR delta / Q000819:agonists*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology
C425931:GW 501516; D006016:Glycolates; D047494:PPAR delta; D013844:Thiazoles; C005446:thiophenoxyacetic acid