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[多种2-(烷基氨基烷基)巯基-5-芳基-1,3,4-恶二唑的合成及药理研究]

[Synthesis and pharmacological study of various 2-(alkylaminoalkyl)mercapto-5-aryl-1,3,4-oxadiazoles].

作者信息

Mazzone G, Bonina F, Arrigo-Reina R

出版信息

Farmaco Sci. 1977 Jun;32(6):414-29.

PMID:872921
Abstract

Work was continued on the pharmacological study of the 1,3,4-oxadiazole nucleus using aroylhydrazines already used for the synthesis of anti-MAO compounds. S-alkylaminoalkyl derivatives of some 2-mercapto-5-aryl-1,3,4-oxadiazoles were prepared bearing in the 5-position a 3,4,5-trimethoxyphenyl, a 3,5-dimethoxy-4-ethoxyphenyl or a 3,4-dihydroxymethylenephenyl radical. When subjected to pharmacological investigation the compounds showed clear hypotensive activity partially antagonized by atropine and antispastic activity on smooth muscle.

摘要

利用已用于合成抗单胺氧化酶化合物的芳酰肼,继续对1,3,4-恶二唑核进行药理学研究。制备了一些2-巯基-5-芳基-1,3,4-恶二唑的S-烷基氨基烷基衍生物,其5-位带有3,4,5-三甲氧基苯基、3,5-二甲氧基-4-乙氧基苯基或3,4-二羟基亚甲基苯基。当对这些化合物进行药理学研究时,它们表现出明显的降压活性,部分被阿托品拮抗,并且对平滑肌有解痉活性。

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