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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
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
Keywords: Analgesic agents; Anti-inflammatory agents; COX-2 inhibitors; Diarylpyrroles; Medicinal chemistry
Issue Date: 2015
Project: None 
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.
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2014.12.041
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