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Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents |
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| Authors: | Humphries Paul S Bailey Simon Almaden Jonathon V Barnum Sandra J Carlson Thomas J Christie Lance C Do Quyen-Quyen T Fraser James D Hess Mary Kellum Jack Kim Young H McClellan Guy A Ogilvie Kathleen M Simmons Brett H Skalitzky Donald Sun Shaoxian Wilhite David Zehnder Luke R |
| Institution: | Department of Diabetes Chemistry, Pfizer Global R&D, 10770 Science Center Drive, San Diego, CA 92121, USA. paul.humphries@pfizer.com |
| 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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