Abstract
The design, synthesis and evaluation of several dual PPARα/γ agonists with three different heterocycles, viz. pyrazolo[4,3-d]pyrimidin-7-one, quinazolin-4-one and benzo[e][1,3]oxazine-4-one for the treatment of type 2 diabetes and associated dyslipidemia are described. Among them, compound 5cb was found to possess a potent dual PPARα/β agonist property. It significantly reversed diabetic hyperglycemia while improving overall lipid homeostasis in preclinical animal models.
Keywords: PPAR, Diabetes, Synthesis, Ethyl 3-(4-aminophenyl)-2-ethoxypropionate, Dyslipidemia and Plasma glucose
Letters in Drug Design & Discovery
Title: Design, Synthesis and Evaluation of Peroxisome Proliferator-Activated Receptor α/βDual Agonists for the Treatment of Type 2 Diabetes
Volume: 4 Issue: 1
Author(s): Saibal Kumar Das, Chandrasekhar Abbineni, Krovvidi Venkata Lakshmi Narasimha Rao, Javed Iqbal, Ravi Krishna Babu and Ranjan Chakrabarti
Affiliation:
Keywords: PPAR, Diabetes, Synthesis, Ethyl 3-(4-aminophenyl)-2-ethoxypropionate, Dyslipidemia and Plasma glucose
Abstract: The design, synthesis and evaluation of several dual PPARα/γ agonists with three different heterocycles, viz. pyrazolo[4,3-d]pyrimidin-7-one, quinazolin-4-one and benzo[e][1,3]oxazine-4-one for the treatment of type 2 diabetes and associated dyslipidemia are described. Among them, compound 5cb was found to possess a potent dual PPARα/β agonist property. It significantly reversed diabetic hyperglycemia while improving overall lipid homeostasis in preclinical animal models.
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Kumar Das Saibal, Abbineni Chandrasekhar, Venkata Lakshmi Narasimha Rao Krovvidi, Iqbal Javed, Krishna Babu Ravi and Chakrabarti Ranjan, Design, Synthesis and Evaluation of Peroxisome Proliferator-Activated Receptor α/βDual Agonists for the Treatment of Type 2 Diabetes, Letters in Drug Design & Discovery 2007; 4 (1) . https://dx.doi.org/10.2174/157018007778992883
DOI https://dx.doi.org/10.2174/157018007778992883 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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