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SYNTHESIS AND EVALUATION OF NOVEL THIAZOLIDINEDIONES FOR ANTI INFLAMMATORY ACTIVITY

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Author(s): Rekha S | Shantharam U | Vineet chandy

Journal: International Research Journal of Pharmacy
ISSN 2230-8407

Volume: 2;
Issue: 9;
Start page: 81;
Date: 2011;
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Keywords: Anti inflammatory | Protein denaturation | Thiazolidinediones | PPARγ

ABSTRACT
The aim of our study was to review on synthesis and various pharmacological activities associated with thaizolidinediones. Thiazolidinediones (TZDs) or glitazones forms a significant class of drugs which exhibit an array of biological activities ranging from anti diabetic, anti-inflammatory, antibacterial, antifungal, antiviral and anticancer. 1, 3-Thiazolidine-2, 4-dione contains basic skeleton of thiazole or thiazolidine. Presence of one carbonyl group in thiazole at 4th position makes it thiazolidine-4-one which is known for various activities, such as anti-inflammatory and presence of another carbonyl group at 2nd position makes it thiazolidine-2, 4-dione which is basically known for its antidiabetic activity. Various studies report the effects of TZDs on the metabolism of lipids, on cell differentiation and on some cardiovascular risk factors. Success of thiazolidinediones (TZDs), the ligand of peroxisome proliferator-activated receptor γ (PPARγ) has generated a lot of interest for new drug discovery. In the present study we were reporting a systematic synthesis of thiazolidinediones analogues. The basic ring of thiazolidinedione was prepared by 1, 3 dipolar cycloaddition reaction using thiourea and monochloroaceticacid. Knoevenagel condensation with substituted aromatic aldehydes was carried out to yield various substituted benzylidenethiazolidine-2, 4-dione. These were subjected to further alkylation and/or substitution reaction to yield our targets compound as described in scheme 1. The synthesized molecules were screened for bovine serum denaturation (in vitro). Characterization was done by using various physicochemical and spectral techniques. All molecules were weakly active in bovine serum denaturation assay.
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