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3-(取代氨基)-1,2,4-苯并噻二嗪1-氧化物衍生物的合成及其降压活性

Synthesis and blood pressure lowering activity of 3-(substituted-amino)-1,2,4-benzothiadiazine 1-oxide derivatives.

作者信息

Dillard R D, Yen T T, Stark P, Pavey D E

出版信息

J Med Chem. 1980 Jul;23(7):717-22. doi: 10.1021/jm00181a003.

Abstract

A series of (substituted amino)-1,2,4-benzothiadiazine 1-oxides has been synthesized and most members of the series have been shown to have blood pressure lowering effects in normotensive rabbits and in spontaneously hypertensive rats. The most active member of the series was 3-[4-(2-furoyl)-1-piperazinyl]-6,7-dimethoxy-1-methyl-1H-1,2,4-benzothiadiazine 1-oxide hydrochloride. This compound in animal tests was equipotent to the known antihypertensive Prazosin.

摘要

已经合成了一系列(取代氨基)-1,2,4-苯并噻二嗪1-氧化物,并且该系列的大多数成员已被证明在正常血压兔和自发性高血压大鼠中具有降血压作用。该系列中最具活性的成员是3-[4-(2-呋喃甲酰基)-1-哌嗪基]-6,7-二甲氧基-1-甲基-1H-1,2,4-苯并噻二嗪1-氧化物盐酸盐。该化合物在动物试验中与已知的抗高血压药哌唑嗪等效。

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