COX-1/COX-2 inhibitors based on the methanone moiety
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Updated: Oct 2, 2026

Structure-Guided Design and Development of Novel Cyclophilin A Inhibitors and Ganoderiol-F Derivatives: An In-Silico Approach
Published on: June 23, 2026
Gerd Dannhardt1, Bernd L Fiebich, Johannes Schweppenhäuser
1Institute of Pharmacy, Fachbereich Chemie und Pharmazie, Johannes Gutenberg University of Mainz, Staudingerweg 5, D-55099 Mainz, Germany. dannhrdt@mail.uni-mainz.de
Abstract:
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- and 4-regioisomers were also investigated. The potency and the enzyme selectivity were varied by structural modifications of the lead.
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