Synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl and sulfamoyl acetamides and ethyl acetates as potent COX-2 inhibitors

We report herein the synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl,sulfamoyl acetamides and ethyl acetates that selectively inhibit cyclooxygenase-2 (COX-2) isoform.Among the newly synthesized compounds, some of them were endowed with a good activity againstCOX-2 and a good selectivity COX-2/COX-1 in vitro as well as a desirable analgesic activity in vivo, provingthat replacement of the ester moiety with an amide group gave access to more stable derivatives,characterized by a good COX-inhibition.