Dual PPAR-alpha and -gamma activators derived from novel benzoxazinone containing thiazolidinediones having antidiabetic and hypolipidemic potential

  • Bioorg Med Chem. 2006 Jan 15;14(2):584-91. doi: 10.1016/j.bmc.2005.08.043.
Gurram R Madhavan  1 ,  Ranjan Chakrabarti ,  K Anantha Reddy ,  B M Rajesh ,  V Balraju ,  P Bheema Rao ,  R Rajagopalan ,  Javed Iqbal
Affiliations
  • 1. Discovery Chemistry, Dr. Reddy's Laboratories Ltd., Bollarum Road, Miyapur, Hyderabad 500049, India. [email protected]
PMID: 16198573 DOI: 10.1016/j.bmc.2005.08.043
Abstract

2,4-Thiazolidinedione derivatives of 1,3-benzoxazinone were synthesized and evaluated for their PPAR-alpha and -gamma dual activation. DRF-2519, a compound obtained through SAR of TZD derivatives of benzoxazinone, has shown potent dual PPAR activation. In ob/ob mice, it showed better efficacy than the comparator molecules. In fat fed rat model, it showed significant improvement in lipid parameters, which was better than fibrates.

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