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Bioorg Med Chem Lett. 2001 May 7;11(9):1225-7.

Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.

Author information

1
GlaxoSmithKline, Research Triangle Park, NC 27709-3398, USA. pjb5890@gsk.com

Abstract

Using solid-phase, parallel-array synthesis, a series of urea-substituted thioisobutyric acids was synthesized and assayed for activity on the human PPAR subtypes. GW7647 (3) was identified as a potent human PPARalpha agonist with approximately 200-fold selectivity over PPARgamma and PPARdelta, and potent lipid-lowering activity in animal models of dyslipidemia. GW7647 (3) will be a valuable chemical tool for studying the biology of PPARalpha in human cells and animal models of disease.

PMID:
11354382
DOI:
10.1016/s0960-894x(01)00188-3
[Indexed for MEDLINE]

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