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

Bioorganicheskaia khimiia Pub Date : 2014-05-01
S A Meshcheriakova, V A Kataev, K V Nikolaeva, V N Perfilova, D D Borodin, I N Tiurenkov
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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.

[尿酰基乙酸含硫酰基肼的合成、异构和降压活性]。
通过肼- 2-[6-甲基-1-(噻吩-3-基)尿嘧啶-3-基]乙酸与芳醛和苯乙酮衍生物的反应,得到了酰基腙,在DMSO溶液中以E(C=N)-异构体的两种立体异构体的混合物存在,由于肼键周围的内旋受阻。结果表明,所合成的化合物具有抗高血压活性。
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