Arylidene analogues as selective COX-2 inhibitors: synthesis, characterization, and studies.

Pyrazole derivatives are known to be as non-steroidal anti-inflammatory drugs (NSAID). is the pioneer sulfonamide being pyrazole derivative COX-2 inhibitors, which used to treat pain and inflammation; they may also have a role in cancer prevention. In the present investigation, a series of arylidene analogues ( to ) were synthesized by the condensation of 4-(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl) benzenesulfonamide () with various substituted aromatic aldehydes in ethanol using a catalytic amount of piperidine. All the synthesized compounds were well characterized by IR, H NMR, C NMR and mass spectrometry. The cytotoxicity of synthesized compounds was tested on the cell line. From which , , , and were found to have higher cytotoxicity whereas showed less cytotoxicity compared to . The pharmacokinetic parameters of compounds were evaluated to check their candidature as a drug. Molecular docking was carried out on COX-2 structures, which revealed that to targets allosteric binding site similar to the binding mode of the selective COX inhibitor . Furthermore, results of COX-2 inhibition assay supports arylidene analogues as COX-2 inhibitors.