Microwave Assisted Synthesis and Anti-HIV-RT Activity of Diaryl Benzo[1,3]thiazin-4-ones

doi:10.6023/cjoc201412053

Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (6): 1370-1374.DOI: 10.6023/cjoc201412053 Previous Articles Next Articles

Notes

二芳基苯并1,3-噻嗪烷-4-酮衍生物的微波促进合成及其HIV逆转录酶抑制活性

冯俊娜^a,b, 李晓慧^c, 邵洁^a, 朱墨^a, 李妍^a, 陈华^a, 李小六^a

a 河北大学化学与环境科学学院河北省化学生物学重点实验室保定 071002;
b 中国地质大学长城学院地球科学与资源系保定 071000;
c 河北农业大学理学院保定 071001

收稿日期:2014-12-30 修回日期:2015-02-03 发布日期:2015-02-05
通讯作者: 陈华, 李小六 E-mail:lixl@hbu.cn;hua-todd@163.com
基金资助:
国家自然科学基金(No. 21372060)、河北省自然科学基金石药集团医药联合基金(No. B2012201113)、河北省教育厅自然科学基金(No. Y2011119)、保定市科技局(No. 14ZF095)资助项目.

Microwave Assisted Synthesis and Anti-HIV-RT Activity of Diaryl Benzo[1,3]thiazin-4-ones

Feng Junna^a,b, Li Xiaohui^c, Shao Jie^a, Zhu Mo^a, Li Yan^a, Chen Hua^a, Li Xiaoliu^a

a Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002;
b Department of the Earth Sciences and Resources, China University of Geosciences Great Wall College, Baoding 071000;
c College of Sciences, Agricultural University of Hebei, Baoding 071001

Received:2014-12-30 Revised:2015-02-03 Published:2015-02-05
Supported by:
Project supported by the National Natural Science Foundation of China (No. 21372060), the Medicinal Joint Funds of the Natural Science Foundation of Hebei and Shijiazhuang Pharmaceutical Group (No. B2012201113), the Natural Science Foundations of Education Department of Hebei (No. Y2011119), and the Foundations of Baoding City Science and Technology Bureau (No. 14ZF095).

1. Microwave Assisted Synthesis and Anti-HIV-RT Activity of Diaryl Benzo[1,3]thiazin-4-ones.PDF(1312KB)

Abstract

A series of novel diaryl benzothiazin-4-ones were designed and synthesized by the three-component one-pot cyclocondensation of pyrimidinamine, aromatic aldehyde and thiosalicylic acid under microwave irradiation for 10 min. The reaction has the advantages such as short reaction time and simple operation. The structures of the newly synthesized compounds were confirmed by IR, NMR, MS spectra and elemental analysis. The compound 2-(2,6-dichlorophenyl)-3-(4,6-di- methylpyrimidin-2-yl)-2H-benzo[e][1,3]thiazin-4(3H)-one (10c) could effectively inhibit HIV-RT activity with the IC₅₀ value of 8.38 祄ol·L^-1, the others showed middle RT inhibitory activity.

Key words: benzothiazin-4-one, anti-HIV-RT activity, microwave irradiation

Cite this article

Feng Junna, Li Xiaohui, Shao Jie, Zhu Mo, Li Yan, Chen Hua, Li Xiaoliu. Microwave Assisted Synthesis and Anti-HIV-RT Activity of Diaryl Benzo[1,3]thiazin-4-ones[J]. Chin. J. Org. Chem., 2015, 35(6): 1370-1374.

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二芳基苯并1,3-噻嗪烷-4-酮衍生物的微波促进合成及其HIV逆转录酶抑制活性

Microwave Assisted Synthesis and Anti-HIV-RT Activity of Diaryl Benzo[1,3]thiazin-4-ones

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