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[1,2,4-苯并噻二嗪-1,1-二氧化物衍生物的心血管作用。VI]

[Cardiovascular action of 1,2,4-benzothiadiazine-1,1-dioxide derivatives. VI].

作者信息

Di Bella M, Pecorari P, Ferrari P, Parenti C, Raffa L, Ferrari W

出版信息

Farmaco Sci. 1978 Feb;33(2):81-91.

PMID:631322
Abstract

A series of 3,4-dihydro derivatives of 6-chloro-, 7-chloro-, 5,7-dichloro-, 6,7-dichloro-, 5,7-dibromo-, 5-nitro-7-chloro-, 7-nitro-, 7-amino-1,2,4-benzothiadiazine-1,1-dioxide, various substituted on the heterocyclic carbon, was prepared and tested for cardiovascular activity. It was found that in this series of compounds cardiac activity predominates and is exclusively of the depressant type. Bradycardial activity seems to be affected both by the nature of the substituent on the heterocyclic carbon atom and by the substituents on the benzene ring. An alkyl chain of three carbon atoms, normal or alpha-ethylsubstituted, on C3 and the presence of a chlorine atom in positions 6 or 7 seem to be the most significant structural features for this activity. Some of the substances tested showed a pressor effect (hypotension and/or increase in differential pressure).

摘要

制备了一系列6-氯-、7-氯-、5,7-二氯-、6,7-二氯-、5,7-二溴-、5-硝基-7-氯-、7-硝基-、7-氨基-1,2,4-苯并噻二嗪-1,1-二氧化物的3,4-二氢衍生物,这些衍生物在杂环碳上有各种取代基,并对其心血管活性进行了测试。结果发现,在这一系列化合物中,心脏活性占主导,且完全是抑制性的。心动过缓活性似乎受到杂环碳原子上取代基的性质以及苯环上取代基的影响。C3上具有三个碳原子的直链或α-乙基取代的烷基链以及6位或7位存在氯原子似乎是该活性最重要的结构特征。一些测试物质显示出升压作用(低血压和/或压差增加)。

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