title: Dual PPAR-alpha and -gamma activators derived from novel benzoxazinone containing thiazolidinediones having antidiabetic and hypolipidemic potential.
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.
authors.affiliation: Discovery Chemistry, Dr. Reddy's Laboratories Ltd., Bollarum Road, Miyapur, Hyderabad 500049, India. madhavangr@rediffmail.com
authors.forename: Gurram R
authors.initials: GR
authors.lastname: Madhavan
authors.forename: Ranjan
authors.initials: R
authors.lastname: Chakrabarti
authors.forename: K Anantha
authors.initials: KA
authors.lastname: Reddy
authors.forename: B M
authors.initials: BM
authors.lastname: Rajesh
authors.forename: V
authors.initials: V
authors.lastname: Balraju
authors.forename: P Bheema
authors.initials: PB
authors.lastname: Rao
authors.forename: R
authors.initials: R
authors.lastname: Rajagopalan
authors.forename: Javed
authors.initials: J
authors.lastname: Iqbal
mesh_terms: D000818:Animals; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D051381:Rats; D017207:Rats, Sprague-Dawley; D045162:Thiazolidinediones / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D047493:PPAR alpha; D047495:PPAR gamma; D045162:Thiazolidinediones