2. Academic Validation
  3. Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents

Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents

  • Bioorg Med Chem Lett. 2006 Dec 1;16(23):6120-3. doi: 10.1016/j.bmcl.2006.08.110.
Paul S Humphries 1,  Simon Bailey,  Jonathon V Almaden,  Sandra J Barnum,  Thomas J Carlson,  Lance C Christie,  Quyen-Quyen T Do,  James D Fraser,  Mary Hess,  Jack Kellum,  Young H Kim,  Guy A McClellan,  Kathleen M Ogilvie,  Brett H Simmons,  Donald Skalitzky,  Shaoxian Sun,  David Wilhite,  Luke R Zehnder
Affiliations

Affiliation

  • 1 Department of Diabetes Chemistry, Pfizer Global R&D, 10770 Science Center Drive, San Diego, CA 92121, USA. paul.humphries@pfizer.com
PMID: 16973358 DOI: 10.1016/j.bmcl.2006.08.110
Abstract

A series of novel pyridine-3-propanoic acids was synthesized. A structure-activity relationship study of these compounds led to the identification of potent dual PPARalpha/gamma agonists with varied isoform selectivity. Based on the results of efficacy studies in diabetic (db/db) mice, and the desired pharmacokinetic parameters, compounds (S)-14 and (S)-19 were selected for further profiling.

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