COX-1/COX-2 inhibitors based on the methanone moiety

…, BL Fiebich, J Schweppenhäuser

文献索引：Dannhardt, Gerd; Fiebich, Bernd L; Schweppenhaeuser, Johannes European Journal of Medicinal Chemistry, 2002 , vol. 37, # 2 p. 147 - 161

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被引用次数: 29

摘要

This paper focuses on the synthesis and the in vitro testing of dual COX-1/COX-2 inhibitors. Starting from structures of non-steroidal anti-inflammatory drugs (NSAIDs) the diaryl methanone element was chosen as a lead. Modifications were carried out on this scaffold to obtain potent inhibitors of the COX enzymes. The N-(2-aroylphenyl) sulphonamides and- amides were studied in detail, and to consolidate the data evaluated the corresponding 3- ...