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

Ling Luo H.; Yang W.; Li Y.; Fan Yin S.

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

机译：含有3,4-二氢嘧啶-2（H）-一和3,4-二氢嘧啶-2（H）-硫酮部分的螺旋衍生物的合成和镇定活性

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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.

机译：从螺旋开始，合成了一系列含有3，4-二氢嘧啶-2（1H）-one和3，4-二氢嘧啶2（1H）-硫酮部分的新型螺旋衍生物（3a-3f和4a-4f）。新化合物的结构通过〜1H NMR，IR和HR-MS光谱表征。使用小鼠的自发运动能力测试，评估目标化合物的镇静催眠活性。所有的衍生物都产生中等至高活性。尤其是，化合物4a与其他衍生物相比，表现出最强的镇静催眠作用，衍生物3a，3c，3d，3e和3f也表现出强大的活性。

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来源
《Chemistry of Natural Compounds》 |2010年第3期|共5页
作者
Ling Luo H.; Yang W.; Li Y.; Fan Yin S.;
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正文语种 eng
中图分类化学;
关键词
3; 4-dihydropyrimidine; Biginelli reaction; helicid; sedative-hypnotic activity;

机译：3;4-二氢嘧啶;Biginelli反应;螺旋体;镇静催眠活性;

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1. Synthesis and calming activity of helicid derivatives containing the 3,4-dihydropyrimidin-2(H)-one and 3,4-dihydropyrimidine-2(H)-thione moiety [J] . Ling Luo H., Yang W., Li Y., Chemistry of Natural Compounds . 2010,第3期

机译：含有3,4-二氢嘧啶-2（H）-一和3,4-二氢嘧啶-2（H）-硫酮部分的螺旋衍生物的合成和镇定活性
2. Simple ultrasound-assisted synthesis of 3,4-dihydropyrimidin-2(1H)-one and 3,4-dihydropyrimidine-2(1H)-thione-fused steroidal derivatives by a three-component reaction [J] . DuttaM., GogoiJ., ShekarraoK., Synthesis: International Journal of Methods in Synthetic Organic Chemistry . 2012,第16期

机译：通过三组分反应简单超声辅助合成3,4-dihydropyrimidin-2（1H）-one和3,4-dihydropyrimidine-2（1H）-thione融合的甾体衍生物
3. The Recyclable Bronsted Acidic Liquid Resin Mediated Eco-benign Synthesis of 3,4-Dihydropyrimidine-2(1H)-ones and 3,4-Dihydropyrimidin-2(1H)-thiones via Biginelli Reaction [J] . D. Parthiban, R. Joel Karunakaran, C. J. Magesh International Research Journal of Pure and Applied Chemistry . 2018,第1期

机译：可循环的布朗斯台德酸性液体树脂通过Biginelli反应介导的3,4-二氢嘧啶-2（1H）-酮和3,4-二氢嘧啶-2（1H）-硫酮的生态友好合成
4. Synthesis and Insecticidal Activity of Novel Dihalopropene Derivatives Containing Benzoxazole Moiety: A Structure-Activity Relationship Study [C] . Aiying Guan, Yunkun Qin, Junfeng Wang, Proceedings of 4th international symposium on pesticides and environmental safety amp; 5th pan Pacific confernce on pesticide science amp; 8th international workshop on crop protection chemistry and regulatory harmonization . 2012

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5. Synthesis, optical, and electrochemical properties of novel phthalocyanine derivatives containing [5]helicene moieties. [D] . Sooksimuang, Thanasat. 2001

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

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