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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||Authors:||Consalvi, Sara
DI CAPUA, Angela
La Motta, Concettina
Di Cesare Mannelli, Lorenzo
|Keywords:||Analgesic agents; Anti-inflammatory agents; COX-2 inhibitors; Diarylpyrroles; Medicinal chemistry||Issue Date:||2015||Project:||None||Journal:||BIOORGANIC & MEDICINAL CHEMISTRY||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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