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[含硫杂环丙烷的尿嘧啶乙酸亚甲基酰肼的合成、异构现象及降压活性]

[Synthesis, isomery, and hypotensive activity of thiethane-containing ylidenehydrazides of uracilylacetic acid].

作者信息

Meshcheriakova S A, Kataev V A, Nikolaeva K V, Perfilova V N, Borodin D D, Tiurenkov I N

出版信息

Bioorg Khim. 2014 May-Jun;40(3):327-34.

Abstract

Using reaction of hydrazide 2-[6-methyl-1-(thiethane3-yl)uracil-3-yl]acetic acid with arylaldehydes and acetophenone derivatives were obtained acylhydrazones, which exist in DMSO solution as a mixture of two stereoisomers of a E(C=N)-isomer for due to hindered internal rotation around the hydrazide bond. It was revealed that the synthesized compounds exhibit antihypertensive activity.

摘要

利用酰肼2-[6-甲基-1-(硫代乙烷-3-基)尿嘧啶-3-基]乙酸与芳醛和苯乙酮衍生物反应得到酰腙,由于酰肼键周围的内旋转受阻,其在二甲基亚砜溶液中以E(C=N)异构体的两种立体异构体的混合物形式存在。结果表明,合成的化合物具有抗高血压活性。

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