Revisiting glitazars: thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodents

  • Bioorg Med Chem Lett. 2011 May 15;21(10):3103-9. doi: 10.1016/j.bmcl.2011.03.020.
Preeti Raval  1 ,  Mukul Jain ,  Amitgiri Goswami ,  Sujay Basu ,  Archana Gite ,  Atul Godha ,  Harikishore Pingali ,  Saurin Raval ,  Suresh Giri ,  Dinesh Suthar ,  Maanan Shah ,  Pankaj Patel
Affiliations
  • 1. Zydus Research Centre, Sarkhej-Bavla N.H 8A Moraiya, Ahmedabad 382210, India. [email protected]
PMID: 21450468 DOI: 10.1016/j.bmcl.2011.03.020
Abstract

In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, novel thiophene substituted oxazole containing α-alkoxy-phenylpropanoic acid derivatives are designed as highly potent PPARα/γ dual agonists. These compounds were found to be efficacious at picomolar concentrations. Lead compound 18d has emerged as very potent PPARα/γ dual agonist demonstrating potent antidiabetic and lipid lowering activity at a very low dose and did not exhibit any significant signs of toxicity in rodents.