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.

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

SARTINI, STEFANIA;LA MOTTA, CONCETTINA;
2015

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.
Consalvi, Sara; Alfonso, Salvatore; Di Capua, Angela; Poce, Giovanna; Pirolli, Adele; Sabatino, Manuela; Ragno, Rino; Anzini, Maurizio; Sartini, Stefania; LA MOTTA, Concettina; Di Cesare Mannelli, Lorenzo; Ghelardini, Carla; Biava, Mariangela
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/778945
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