Synthesis, Antidiabetic Evaluation and Molecular Docking Studies of Thiazolidine-2,4-Dione Analogues
نویسندگان
چکیده
Abstract: Introduction: Diabetes Mellitus is a disorder of metabolism described by high glucose levels. The kills larger number individuals consistently than malignant growth and AIDS combined. Presently available drugs have several drawbacks forcing to withdraw from treatment. potent side effect i.e., hepatotoxicity cardiovascular toxicity limits the use thiazolidine-2,4-dione derivative as safe drugs. Our aim towards development synthetic compounds potential antidiabetic agents, particularly preparation screening new analogues (TZD) which are well established oral insulin sensitizing agents that improve resistance agonists Peroxisome Proliferator Activated Receptor–γ (PPAR-γ). Materials Methods: Proper substitution at C-5 position could produce better antidiabetics with improved pharmacological properties, including toxicity. this research work this. Results: A series substituted were synthesized. Structures these confirmed IR, 1H-NMR MASS spectroscopy. Among synthesized compounds, three compounds: 5-(2-pyridinylbenzylidene) thiazolidine-2,4-dione, 5-(3,4-dimethoxybenzylidene) 5-(2,3,4-trifluorobenzylidene) showed significant activity in streptozotocin induced diabetic mice comparable Pioglitazone drug. molecular docking studies performed using protein target amino acid interactions Leu270, Gln283 Arg288 similar Rosiglitazone Pioglitazone. did not show any toxic even 2000 mg/kg dose. Therefore, synthesis modified containing other currently importance drug research. Keywords: Thiazolidine-2,4-dione, Molecular docking, Antidiabetic evaluation, Swiss albino mice.
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ژورنال
عنوان ژورنال: Indian Journal of Pharmaceutical Education and Research
سال: 2023
ISSN: ['0019-5464']
DOI: https://doi.org/10.5530/ijper.57.1s.11