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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。VII]

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

作者信息

Di Bella M, Ferrari P, Pizzirani V, Parenti C, Raffa L

出版信息

Farmaco Sci. 1978 May;33(5):350-9.

PMID:738452
Abstract

A series of dimethylamino-, diethylamino-, pyrrolidyl- and morpholylalkyl derivatives of 3-amino-1,2,4-benzothiadiazine-1,1-dioxide (compounds I leads to XX) was prepared and tested for cardiovascular activity. It was found that substitution of the alkyl group with the above mentioned groups in 3-amino-1,2,4-benzothiadiazine-1,1-dioxide derivatives in most cases causes marked dissociation of hypotensive activity from bradycardial activity and also disappearance or great reduction in the effect on differential pressure. It was also found that hypotensive activity is particularly dependent on the nature of the basic chain in the two components: length of the carbon chain between the two nitrogens and nature of the basic grouping. For the first component a chain of three carbon atoms seems the most effective and for the second the diethylamino group seems the most favourable. In addition, substituents in the benzene ring influence hypotensive activity, often positively, and 6,7-dichlorosubstitution in some compounds also affects the increase of differential pressure.

摘要

制备了一系列3-氨基-1,2,4-苯并噻二嗪-1,1-二氧化物的二甲基氨基、二乙氨基、吡咯烷基和吗啉基烷基衍生物(化合物I至XX),并对其心血管活性进行了测试。结果发现,在3-氨基-1,2,4-苯并噻二嗪-1,1-二氧化物衍生物中,用上述基团取代烷基在大多数情况下会导致降压活性与心动过缓活性明显解离,同时对压差的影响也消失或大幅降低。还发现,降压活性特别取决于两个组分中碱性链的性质:两个氮原子之间碳链的长度和碱性基团的性质。对于第一个组分,三个碳原子的链似乎最有效,对于第二个组分,二乙氨基似乎最有利。此外,苯环上的取代基通常对降压活性有积极影响,某些化合物中的6,7-二氯取代也会影响压差的增加。

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