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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Design and Synthesis of Novel 1,3-Dioxane-2-carboxylic Acid Derivatives as PPARα/γ Dual Agonists

Author(s): Harikishore Pingali, Mukul Jain, Shailesh Shah, Pankaj Makadia, Pandurang Zaware, Jeevankumar Jamili, Kalapatapu V.V.M. Sairam, Pravin Patil, Dinesh Suthar, Suresh Giri, Harilal Patel and Pankaj Patel

Volume 7, Issue 6, 2010

Page: [421 - 429] Pages: 9

DOI: 10.2174/157018010791306533

Price: $65

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Abstract

1,3-dioxane carboxylic acid derivatives were prepared based on our previous studies directed towards identifying novel pharmacophore for the development of PPAR α/γ dual agonists. Based on the typical topology of PPAR agonists we focused our design approach on modifying lipophilic tail and prepared a series of compounds by replacing the oxazole moiety of our previously reported compound with optimized lipophilic groups. Compound 8a was found to be a weak PPAR activator but exhibited potent hypolipidemic and anti-hyperglycemic activities in vivo due to superior bioavailability, whereas 8f exhibited potent in vitro and invivo effects. The activity of 8f is further supported by molecular docking study.

Keywords: PPAR agonist, PPAR α/γ dual agonists, Type 2 diabetes, 1,3-dioxane carboxylic acid


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