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新型1,2,4-恶二唑衍生物:合成及肾上腺素能受体结合研究

New 1,2,4-oxadiazole derivatives: synthesis and adrenergic receptors binding studies.

作者信息

Brizzi V, Brufani M, Filocamo L, Bruni G, Fiaschi A I

机构信息

Dipartmento Farmaco-Chimico-Tecnologico, Università Di Siena.

出版信息

Farmaco. 1992 Jun;47(6):953-66.

PMID:1326978
Abstract

In order to obtain derivatives with simultaneous alpha- and beta-adrenergic blocking activity, compounds having the phenoxypropanolaminic structure of beta-adrenergic blockers have been synthesised, as well as 1,2,4-oxadiazole moiety, which could imitate the imidazolinic nucleus characteristic of drugs acting on alpha-adrenergic receptors. The synthesised compounds have been submitted to alpha and beta receptor binding assays. Some derivatives showed an alpha-adrenoceptor binding activity higher than labetalol and similar to prazosin, but with a poor beta-adrenoceptor binding activity.

摘要

为了获得同时具有α和β肾上腺素能阻断活性的衍生物,已经合成了具有β肾上腺素能阻滞剂苯氧丙醇胺结构的化合物,以及1,2,4-恶二唑部分,其可以模拟作用于α肾上腺素能受体的药物的咪唑啉核特征。已对合成的化合物进行α和β受体结合试验。一些衍生物显示出高于拉贝洛尔且与哌唑嗪相似的α肾上腺素能受体结合活性,但β肾上腺素能受体结合活性较差。

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