Volume 33, Issue 8
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ChemInform Abstract: Identification of a Series of PPARγ/δ Dual Agonists via Solid-Phase Parallel Synthesis.

Kevin G. Liu

Kevin G. Liu

Nucl. Recept. Discovery Res., GlaxoSmithKline, Research Triangle Park, NC 27709, USA

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Millard H. Lambert

Millard H. Lambert

Nucl. Recept. Discovery Res., GlaxoSmithKline, Research Triangle Park, NC 27709, USA

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Lisa M. Leesnitzer

Lisa M. Leesnitzer

Nucl. Recept. Discovery Res., GlaxoSmithKline, Research Triangle Park, NC 27709, USA

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William Oliver Jr.

William Oliver Jr.

Nucl. Recept. Discovery Res., GlaxoSmithKline, Research Triangle Park, NC 27709, USA

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Ronda J. Ott

Ronda J. Ott

Nucl. Recept. Discovery Res., GlaxoSmithKline, Research Triangle Park, NC 27709, USA

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Kelli D. Plunket

Kelli D. Plunket

Nucl. Recept. Discovery Res., GlaxoSmithKline, Research Triangle Park, NC 27709, USA

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Ludwig W. Stuart

Ludwig W. Stuart

Nucl. Recept. Discovery Res., GlaxoSmithKline, Research Triangle Park, NC 27709, USA

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Peter J. Brown

Peter J. Brown

Nucl. Recept. Discovery Res., GlaxoSmithKline, Research Triangle Park, NC 27709, USA

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Timothy M. Willson

Timothy M. Willson

Nucl. Recept. Discovery Res., GlaxoSmithKline, Research Triangle Park, NC 27709, USA

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Daniel D. Sternbach

Daniel D. Sternbach

Nucl. Recept. Discovery Res., GlaxoSmithKline, Research Triangle Park, NC 27709, USA

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First published: 22 May 2010

Abstract

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ChemInform Abstract

A general solid-phase synthesis for identification of PPAR ligands is developed. The synthesis of a 480-member library led to the identification of the potent PPAR γ/δ dual agonist (I). (I) shows good plasma exposure in rats and demonstrates antihyperglycemic and antihyperlipidemic efficacy in diabetic rats.

chemical structure image

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