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