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

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

Affiliation

  • 1 Zydus Research Centre, Sarkhej-Bavla N.H 8A Moraiya, Ahmedabad 382210, India. preetiraval@zyduscadila.com
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.

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