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  • Title: Synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl and sulfamoyl acetamides and ethyl acetates as potent COX-2 inhibitors.
    Author: Consalvi S, Alfonso S, Di Capua A, Poce G, Pirolli A, Sabatino M, Ragno R, Anzini M, Sartini S, La Motta C, Di Cesare Mannelli L, Ghelardini C, Biava M.
    Journal: Bioorg Med Chem; 2015 Feb 15; 23(4):810-20. PubMed ID: 25596758.
    Abstract:
    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 against COX-2 and a good selectivity COX-2/COX-1 in vitro as well as a desirable analgesic activity in vivo, proving that replacement of the ester moiety with an amide group gave access to more stable derivatives, characterized by a good COX-inhibition.
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