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2-(4-芳基硫代氨基脲羰基硫代)苯并噻唑的合成及其单胺氧化酶抑制和抗惊厥特性

Synthesis of 2-(4-arylthiosemicarbazidocarbonylthio)benzthiazoles and their monoamine oxidase inhibitory and anticonvulsant properties.

作者信息

Singh S P, Misra R S, Parmar S S, Brumleve S J

出版信息

J Pharm Sci. 1975 Jul;64(7):1245-7. doi: 10.1002/jps.2600640730.

Abstract

Ten 2-(4-arylthiosemicarbazidocarbonylthio)benzthiazoles were synthesized, characterized, and evaluated for their monoamine oxidase inhibitory and anticonvulsant activities. All substituted benzthiazoles inhibited activity of monoamine oxidase in rat brain homogenate where the degree of enzyme inhibition was higher with kynuramine as compared to tyramine and 5-hydroxytryptamine as the substrates. All substituted benzthiazoles possessed measurable anticonvulsant activity against pentylenetetrazol-induced convulsions.

摘要

合成了十种2-(4-芳基硫代氨基脲羰基硫代)苯并噻唑,对其进行了表征,并评估了它们的单胺氧化酶抑制和抗惊厥活性。所有取代的苯并噻唑均抑制大鼠脑匀浆中单胺氧化酶的活性,其中以犬尿胺为底物时酶抑制程度高于以酪胺和5-羟色胺为底物时。所有取代的苯并噻唑对戊四氮诱导的惊厥均具有可测量的抗惊厥活性。

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