Discovery and SAR of para-alkylthiophenoxyacetic acids as potent and selective PPARdelta agonists

Rui Zhang; Alan Deangelis; Aihua Wang; Ellen Sieber-McMaster; Xun Li; Ronald Russell; Patricia Pelton; Jun Xu; Peifang Zhu; Lubing Zhou; Keith Demarest; William V Murray; Gee-Hong Kuo

doi:10.1016/j.bmcl.2008.12.113

Discovery and SAR of para-alkylthiophenoxyacetic acids as potent and selective PPARdelta agonists

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1101-4. doi: 10.1016/j.bmcl.2008.12.113. Epub 2009 Jan 8.

Authors

Rui Zhang¹, Alan Deangelis, Aihua Wang, Ellen Sieber-McMaster, Xun Li, Ronald Russell, Patricia Pelton, Jun Xu, Peifang Zhu, Lubing Zhou, Keith Demarest, William V Murray, Gee-Hong Kuo

Affiliation

¹ Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, LLC, 8 Clarke Drive, Cranbury, NJ 08512, USA. rzhang4@prdus.jnj.com

PMID: 19168353
DOI: 10.1016/j.bmcl.2008.12.113

Abstract

Synthesis and SAR of para-alkylthiophenoxyacetic acids is described. Achiral compounds 30, 31 and 32 were identified as potent and selective PPARdelta agonists.

MeSH terms

Combinatorial Chemistry Techniques
Drug Design
Drug Discovery
Drug Evaluation, Preclinical
Glycolates / chemical synthesis*
Glycolates / chemistry
Glycolates / pharmacology*
Humans
Models, Molecular
Molecular Structure
PPAR delta / agonists*
Stereoisomerism
Structure-Activity Relationship
Thiazoles / pharmacology

Substances

GW 501516
Glycolates
PPAR delta
Thiazoles
thiophenoxyacetic acid