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2013 , Vol. 33 >Issue 07: 1478 - 1482

DOI: https://doi.org/10.6023/cjoc201212026

研究论文

4-烷基-6-芳基-1,3-噻嗪的合成与生物活性

  • 李婉 ,
  • 胡艾希 ,
  • 刘艾林 ,
  • 彭俊梅 ,
  • 夏林 ,
  • 谭卫清
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  • a 湖南大学化学化工学院 长沙 410082;
    b 中国医学科学院药物研究所 北京 010

收稿日期: 2012-12-17

  修回日期: 2013-03-02

  网络出版日期: 2013-03-06

基金资助

国家教育部博士点专项基金(No. 20040532002)资助项目.

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Synthesis and Biological Activities of 4-Alkyl-6-aryl-1,3-thiazines

  • Li Wan ,
  • Hu Aixi ,
  • Liu Ailin ,
  • Peng Junmei ,
  • Xia Lin ,
  • Tan Weiqing
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  • a College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082;
    b Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050

Received date: 2012-12-17

  Revised date: 2013-03-02

  Online published: 2013-03-06

Supported by

Project supported by the Ph.D. Programs Foundation of Ministry of Education of China (No. 20040532002).

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摘要

以芳香醛为原料, 经缩合、环化等合成了16种1,3-噻嗪化合物1a～1p, 并对其进行了体外神经氨酸酶(NA)和5-羟色胺转运体(SERT)抑制活性测试, 测试结果显示部分化合物对神经氨酸酶和5-羟色胺转运体有抑制活性. 其中化合物1i在40 μg/mL浓度下对神经氨酸酶的抑制率达68.91%, 10 μg/mL浓度下, 1d, 1e和1f对5-羟色胺转运体的抑制率分别为99.5%, 99.6%和99.8%.

关键词： 合成; 1,3-噻嗪; 神经氨酸酶抑制剂; 5-羟色胺转运体抑制剂

本文引用格式

李婉 , 胡艾希 , 刘艾林 , 彭俊梅 , 夏林 , 谭卫清 . 4-烷基-6-芳基-1,3-噻嗪的合成与生物活性[J]. 有机化学, 2013 , 33(07) : 1478 -1482 . DOI: 10.6023/cjoc201212026

Abstract

A series of 1,3-thiazine derivatives 1a～1p were designed and synthesized by the reaction of aromatic aldehyde via condensation and cyclization, and their inhibitory activity of nueraminidase (NA) and serotonin reuptake (SERT) were evaluated in vitro. The pharmacological results showed that compound 1i exhibits good activity of NA with the inhibitory rate of 68.91% at the concentration of 40 μg/mL, which is similar to oseltamivir (inhibitory rate is 72.6%), moreover, at the concentration of 10.0 μg/mL, compounds 1d, 1e and 1f exhibit good serotonin reuptake inhibitory activity with inhibitory rates of 99.5%, 99.6% and 99.8%, respectively.

Key words： synthesis; 1,3-thiazine; neuraminidase inhibitors; serotonin transportor inhibitors

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