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
Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma 'La Sapienza', Piazzale Aldo Moro 5, 00185 Roma, Italy.
Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. De Gasperi, 2, 53100 Siena, Italy.
Bioorg Med Chem. 2015 Feb 15;23(4):810-20. doi: 10.1016/j.bmc.2014.12.041. Epub 2014 Dec 26.
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.
我们在此报告了一系列新型甲基磺酰基、氨磺酰基乙酰胺和乙酸乙酯的合成、生物学评价及对接分析，这些化合物可选择性抑制环氧合酶-2（COX-2）同工型。在新合成的化合物中，其中一些在体外对COX-2具有良好活性及良好的COX-2/COX-1选择性，在体内也具有理想的镇痛活性，这证明用酰胺基团取代酯部分可得到更稳定的衍生物，其特点是具有良好的COX抑制作用。
