Synthesis, Characterization and Biological Evaluation of Novel Coumarins as Promising Anti-Inflammatory Agents

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In the present study, coumarins were synthesized by reaction of substituted phenols and ethyl acetoacetate in the presence of concentrated sulphuric acid (Pechmann reaction)and substituted with different electro-positive and electronegative groups. The binding affinity of compounds was evaluated by molecular docking in the binding site of phospho-diestrase 4 (PDE4) protein using AutoDockVina and dock scores were calculated. The compounds with good binding affinity were screened for the anti-inflammatory activity using carrageenan induced rat paw edema method. Docking studies showed that compounds 3(d-k) have good binding affinity with PDE4. Further, pharmacological investigation revealed that compound 3(d-e) exhibited highest antiinflammatory activity.

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