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Chinese Journal of Organic Chemistry >

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

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

Articles

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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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

Cite this article

Li Wan , Hu Aixi , Liu Ailin , Peng Junmei , Xia Lin , Tan Weiqing . Synthesis and Biological Activities of 4-Alkyl-6-aryl-1,3-thiazines[J]. Chinese Journal of Organic Chemistry, 2013 , 33(07) : 1478 -1482 . DOI: 10.6023/cjoc201212026

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