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不对称1,4-二取代哌嗪的合成及其精神和心血管作用。第二部分。

Synthesis of asymmetric 1,4-disubstituted piperazines and their psychotropic and cardiovascular actions. Part II.

作者信息

Korzycka L, Białasiewicz W, Szadowska A, Darzynkiewicz-Czernik D, Kiełek M

出版信息

Pol J Pharmacol Pharm. 1986 Sep-Dec;38(5-6):545-53.

PMID:3575170
Abstract

New asymmetric piperazines 9-19 were obtained by condensation of 1-acyl-piperazines with 1,2-epoxy-3-chloropropane, arylacid chlorides, phenols, amines and 1-(alpha-naphthyloxy)-2,3-epoxypropane. Most of the compounds produced a transient hypotension and exerted a spasmolytic action of the isolated intestine. Compounds 10, 11 and 13 displayed a weak antiarrhythmic effect in the adrenaline arrhythmia test in rats. Compounds 14 and 15 increased the coronary flow, but their action was weaker than that of compound 4, described in the first part of the paper.

摘要

通过使1-酰基哌嗪与1,2-环氧-3-氯丙烷、芳酰氯、酚类、胺类以及1-(α-萘氧基)-2,3-环氧丙烷缩合,得到了新型不对称哌嗪9-19。大多数化合物产生短暂性低血压,并对离体肠管发挥解痉作用。在大鼠肾上腺素性心律失常试验中,化合物10、11和13表现出微弱的抗心律失常作用。化合物14和15可增加冠脉血流量,但其作用比本文第一部分所述的化合物4弱。

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