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 / 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. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 23:4(2015), pp. 810-820. [10.1016/j.bmc.2014.12.041]

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

CONSALVI, SARA;ALFONSO, SALVATORE;POCE, Giovanna;PIROLLI, ADELE;SABATINO, MANUELA;RAGNO, Rino;BIAVA, Mariangela
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.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/869904
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