Inhibition of monoamine oxidases by functionalized coumarin derivatives: biological activities, QSARs, and 3D-QSARs

…, M Catto, F Leonetti, P Weber, PA Carrupt…

文献索引：Gnerre; Catto; Leonetti; Weber; Carrupt; Altomare; Carotti; Testa Journal of Medicinal Chemistry, 2000 , vol. 43, # 25 p. 4747 - 4758

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被引用次数: 206

摘要

A large series of coumarin derivatives (71 compounds) were tested for their monoamine oxidase A and B (MAO-A and MAO-B) inhibitory activity. Most of the compounds acted preferentially on MAO-B with IC50 values in the micromolar to low-nanomolar range; high inhibitory activities toward MAO-A were also measured for sulfonic acid esters. The most active compound was 7-[(3, 4-difluorobenzyl) oxy]-3, 4-dimethylcoumarin, with an IC50 ...