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Dual PPAR-alpha and -gamma activators derived from novel benzoxazinone containing thiazolidinediones having antidiabetic and hypolipidemic potential
Authors:Madhavan Gurram R  Chakrabarti Ranjan  Reddy K Anantha  Rajesh B M  Balraju V  Rao P Bheema  Rajagopalan R  Iqbal Javed
Institution:Discovery Chemistry, Dr. Reddy's Laboratories Ltd., Bollarum Road, Miyapur, Hyderabad 500049, India. madhavangr@rediffmail.com
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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