Inhibition of monoamine oxidases by coumarin-3-acyl derivatives: biological activity and computational study

…, A Bolasco, P Chimenti, A Granese, O Befani…

文献索引：Chimenti, Franco; Secci, Daniela; Bolasco, Adriana; Chimenti, Paola; Granese, Arianna; Befani, Olivia; Turini, Paola; Alcaro, Stefano; Ortuso, Francesco Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 14 p. 3697 - 3703

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被引用次数: 87

摘要

A series of coumarin-3-acyl derivatives have been synthesized and investigated for the ability to inhibit selectively monoamine oxidases. The coumarin-3-carboxylic acids, 2a–e, proved to be reversible and selective inhibitors of the MAO-B isoform, displaying pIC50 values of particular interest: 2a shows pIC50 7.76 and a selectivity index (pS. I.) 2.94 and 2b shows pIC50 7.72 and a pS. I. of 2.80. The coumarin-3-acyl chlorides 3a–e showed high ...