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取代恶二唑硫酮的抗惊厥和单胺氧化酶抑制活性。

Anticonvulsant and monoamine oxidase inhibitory activity of substituted oxadiazol-thiones.

作者信息

Tripathi S, Ahmad S, Barthwal J P, Tangri K K, Bhargava K P

出版信息

Indian J Physiol Pharmacol. 1982 Apr-Jun;26(2):113-8.

PMID:7141616
Abstract

Several 1,3,4-oxadiazol-thiones were synthesised and characterized by their melting points elemental analysis and I.R. spectra. All the oxadiazol-thiones possessed anticonvulsant activity which was reflected by protection upto 80% against pentylenetetrazole induced seizures and 40% protection against maximal electroshock induced seizures. Substantiations at position-3 of oxadiazol-thiones have shown marked effect on MAO inhibitory activity. No definite correlation between monoamine oxidase inhibitory and anticonvulsant activity could be established. It was observed that by the substitution of one, two and three methyl groups in the phenyl ring of 2-arylamino methyl side chain anticonvulsant activity against both maximal electroshock induced convulsions and pentylenetetrazol induced convulsions decreases i.e. the order of activity was found to be unsubstituted greater than monomethyl greater than dimethyl greater than trimethyl.

摘要

合成了几种1,3,4-恶二唑硫酮,并通过熔点、元素分析和红外光谱对其进行了表征。所有恶二唑硫酮都具有抗惊厥活性,这表现为对戊四氮诱导的惊厥有高达80%的保护作用,对最大电休克诱导的惊厥有40%的保护作用。恶二唑硫酮3位的取代基对单胺氧化酶抑制活性有显著影响。单胺氧化酶抑制活性与抗惊厥活性之间未发现明确的相关性。观察到,在2-芳基氨基甲基侧链的苯环中取代一个、两个和三个甲基后,对最大电休克诱导的惊厥和戊四氮诱导的惊厥的抗惊厥活性均降低,即活性顺序为未取代的大于单甲基的大于二甲基的大于三甲基的。

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