1,3,4-Oxadiazol-2-ylbenzenesulfonamides as privileged structures for the inhibition of monoamine oxidase B.

Anton Shetnev, Roman Shlenev,Julia Efimova, Sergey Ivanovskii, Alexey Tarasov,Anél Petzer,Jacobus P Petzer

Bioorganic & Medicinal Chemistry Letters（2019）

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摘要

•First report of nanomolar MAO inhibition recorded for sulfonamide derivatives.•Most potent MAO-B inhibitor exhibit an IC50 of 0.0027 µM.•High degree of selectivity for MAO-B over MAO-A.•Extensive hydrogen bonding to MAO-B predicted for the sulfonamide functional group.

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关键词

Monoamine oxidase,MAO,Inhibition,Sulfonamide,Zonisamide,Oxadiazole

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