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ISSN 2063-5346
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SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3, 6 DI-SUBSTITUTED 1-BENZOPYRAN-4-ONE ANALOGS AS ANTI-INFLAMMATORY AGENTS.

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Jilla Soujanya[a]*, Dr. D. Ravisankar Reddy

Abstract

A series of 3, 6 di substituted-7-hydroxy-2-methyl-4H-1-benzopyran-4-one derivatives (Chromone Biheterocycles) were synthesized and their structures were established on the basis of modern analytical techniques (1HNMR, 13CNMR and HRMS). All the synthesized compounds were tested for their in vitro anti-inflammatory activity. Among the 21 Synthesized derivatives, Pyrazole linked benzopyran-4-one derivative Compound 7s (IC50= 23.14), Imidazole linked benzopyran-4-one derivatives Compounds 7g (IC 50= 17.52) and 7k (IC50= 19.68) have significant anti-inflammatory activity in comparison with the Diclofenac as control standard (IC50= 16.23). Further demonstrated the mechanism of anti-inflammatory activity for the compounds 7g (2 IC50= 13.5) and 7k (2 IC50= 17.1) using TNF-α ELISA based assay in comparison with the Infliximab (IC50= 12.9) as control standard. Animal experiments were carried out to find the in-vivo efficacy of compound 7g through carrageenan-induced rat paw edema assay method. The results demonstrated that Compound (7g) had significant anti‐inflammatory activity at doses of 50 and 75 mg/kg, had the best significant reduction and inhibition of edema with 82.28, 88.61% and 84.34, 91.57% at third hour and fourth hour respectively, and similar as compared with standard drug Diclofenac 50 mg/kg body weight (p < 0.05). Molecular docking interactions of Compound 7g with TNF-α (2AZ5) using glide protocol of Schrodinger suite revealed best possible pose with a dock score of 9.6. Altogether, our findings suggest that Compound 7g is a promising anti-inflammatory drug candidate, in the management of inflammation and pain conditions.

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