Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (07): 1478-1482.DOI: 10.6023/cjoc201212026 Previous Articles     Next Articles



李婉a, 胡艾希a, 刘艾林b, 彭俊梅a, 夏林a, 谭卫清a   

  1. 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 发布日期:2013-03-06
  • 通讯作者: 胡艾希, 刘艾林;
  • 基金资助:

    国家教育部博士点专项基金(No. 20040532002)资助项目.

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

Li Wana, Hu Aixia, Liu Ailinb, Peng Junmeia, Xia Lina, Tan Weiqinga   

  1. 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:2012-12-17 Revised:2013-03-02 Published:2013-03-06
  • Supported by:

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

A series of 1,3-thiazine derivatives 1a1p 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