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噻吩二氮䓬和苯二氮䓬衍生物的构效关系。

Structure-activity relationships in thienodiazepine and benzodiazepine derivatives.

作者信息

Chimirri A, Gitto R, Grasso S, Zappalà M, De Sarro A, Battista De Sarro G

机构信息

Dipartimento Farmaco-Chimico, Università di Messina, Italy.

出版信息

Farmaco. 1994 Mar;49(3):193-6.

PMID:8043171
Abstract

The structural and electronic characteristics as well as the anticonvulsant properties and benzodiazepine receptor binding of thieno[3,4-b][1,4]diazepine and 1,5-benzodiazepine derivatives are compared and discussed. The data obtained suggest that the electronic rather than the structural properties appear mainly responsible for the variant degree of anticonvulsant activity exhibited by the tested compounds.

摘要

比较并讨论了噻吩并[3,4 - b][1,4]二氮杂䓬和1,5 - 苯二氮杂䓬衍生物的结构和电子特性、抗惊厥特性以及苯二氮䓬受体结合情况。所获得的数据表明,对于受试化合物所表现出的不同程度的抗惊厥活性,起主要作用的似乎是电子特性而非结构特性。

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