Literature DB >> 16198573

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

Gurram R Madhavan1, Ranjan Chakrabarti, K Anantha Reddy, B M Rajesh, V Balraju, P Bheema Rao, R Rajagopalan, Javed Iqbal.   

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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Year:  2005        PMID: 16198573     DOI: 10.1016/j.bmc.2005.08.043

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  11 in total

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2.  Peroxisome Proliferator-Activated Receptors as Superior Targets for Treating Diabetic Disease, Design Strategies - Review Article.

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3.  Rhoda-Electrocatalyzed Bimetallic C-H Oxygenation by Weak O-Coordination.

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Review 4.  Diabetes and hypertension: is there a common metabolic pathway?

Authors:  Bernard M Y Cheung; Chao Li
Journal:  Curr Atheroscler Rep       Date:  2012-04       Impact factor: 5.113

Review 5.  Recent pharmacological developments on rhodanines and 2,4-thiazolidinediones.

Authors:  Ravinder Singh Bhatti; Sakshi Shah; Pawan Krishan; Jagir S Sandhu
Journal:  Int J Med Chem       Date:  2013-05-02

6.  Novel Benzylidene Thiazolidinedione Derivatives as Partial PPARγ Agonists and their Antidiabetic Effects on Type 2 Diabetes.

Authors:  Sabina Yasmin; Fabio Capone; Antonio Laghezza; Fabrizio Dal Piaz; Fulvio Loiodice; Viswanathan Vijayan; Velmurugan Devadasan; Susanta K Mondal; Özlem Atlı; Merve Baysal; Ashok K Pattnaik; Venkatesan Jayaprakash; Antonio Lavecchia
Journal:  Sci Rep       Date:  2017-10-31       Impact factor: 4.379

Review 7.  Targeting Peroxisome Proliferator-Activated Receptors Using Thiazolidinediones: Strategy for Design of Novel Antidiabetic Drugs.

Authors:  Neelaveni Thangavel; Mohammed Al Bratty; Sadique Akhtar Javed; Waquar Ahsan; Hassan A Alhazmi
Journal:  Int J Med Chem       Date:  2017-06-05

8.  Recyclable Keggin Heteropolyacids as an Environmentally Benign Catalyst for the Synthesis of New 2-Benzoylamino-N-phenyl-benzamide Derivatives under Microwave Irradiations at Solvent-Free Conditions and the Evaluation of Biological Activity.

Authors:  Karima Ighilahriz-Boubchir; Baya Boutemeur-Kheddis; Cherifa Rabia; Malika Makhloufi-Chebli; Maamar Hamdi; Artur M S Silva
Journal:  Molecules       Date:  2017-12-21       Impact factor: 4.411

9.  Base-Promoted Chemodivergent Formation of 1,4-Benzoxazepin-5(4H)-ones and 1,3-Benzoxazin-4(4H)-ones Switched by Solvents.

Authors:  Qian Chen; Yunpeng Wang; Ruimao Hua
Journal:  Molecules       Date:  2019-10-19       Impact factor: 4.411

10.  Synthesis, Biological Evaluation and Docking Analysis of Some Novel Quinazolin Derivatives as Antitumor Agents.

Authors:  Walaa S El-Serwy; Neama A Mohamed; Emad M M Kassem; Khaled Mahmoud; M M Mounier
Journal:  Iran J Pharm Res       Date:  2016       Impact factor: 1.696

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