Synthesis and calming activity of helicid derivatives containing the 3,4-dihydropyrimidin-2(H)-one and 3,4-dihydropyrimidine-2(H)-thione moiety

被引：0

作者：

Ling Luo H. ^{[1
]}

Yang W. ^{[1
]}

Li Y. ^{[1
]}

Fan Yin S. ^{[1
]}

机构：

[1] College of Chemistry, Sichuan University

来源：

Chemistry of Natural Compounds | 2010年 / 46卷 / 3期

关键词：

3,4-dihydropyrimidine; Biginelli reaction; helicid; sedative-hypnotic activity;

D O I：

10.1007/s10600-010-9630-5

中图分类号：

学科分类号：

摘要：

A series of novel helicid derivatives containing 3,4-dihydropyrimidin-2(1H) -one and 3,4-dihydropyrimidine2(1H)-thione moiety (3a-3f and 4a-4f) were synthesized starting from helicid. The structure of the new compounds were characterized by 1H NMR, IR and HR-MS spectra. The sedative-hypnotic activities of the target compounds were evaluated using the test of spontaneous locomotor activity in mice. All of the derivatives produced moderate to high activities; in particular, compound 4a presented the most potent sedative-hypnotic effect in comparison to the other derivatives, and derivatives 3a, 3c, 3d, 3e and 3f also showed potent activities. © 2010 Springer Science+Business Media, Inc.

引用

页码：412 / 416

页数：4

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