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

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

  • Bioorg Med Chem Lett. 2001 May 7;11(9):1225-7. doi: 10.1016/s0960-894x(01)00188-3.
P J Brown 1,  L W Stuart,  K P Hurley,  M C Lewis,  D A Winegar,  J G Wilson,  W O Wilkison,  O R Ittoop,  T M Willson
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PMID: 11354382 DOI: 10.1016/s0960-894x(01)00188-3
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.

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