Synthesis and Biological Activities of Novel Substituted-pyrazole 1,2,4-Triazolo[3,4-b]benzothiazole

doi:10.6023/cjoc201210012

Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (05): 1015-1021.DOI: 10.6023/cjoc201210012 Previous Articles Next Articles

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含吡唑取代基的1,2,4-三唑[3,4-b]-1,3,4-噻二唑类衍生物的合成及生物活性

姚明星^a, 安悦^a, 闫杰^a, 田星^b, 魏诗^c

a 辽宁师范大学化学化工学院大连 116029;
b 辽宁师范大学分析测试中心大连 116029;
c 辽宁师范大学化学生命科学大连 116029

收稿日期:2012-10-11 修回日期:2013-01-17 发布日期:2013-01-21
通讯作者: 安悦,anyue_11@163.com E-mail:anyue_11@163.com
基金资助:
辽宁省教育厅基金(No. 2008349)资助项目.

Synthesis and Biological Activities of Novel Substituted-pyrazole 1,2,4-Triazolo[3,4-b]benzothiazole

Yao Mingxing^a, An Yue^a, Yan Jie^a, Tian Xing^b, Wei Shi^c

a School of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029;
b Analysis and Inspection Center, Liaoning Normal University, Dalian 116029;
c School of Life Sciences, Liaoning Normal University, Dalian 116029

Received:2012-10-11 Revised:2013-01-17 Published:2013-01-21
Supported by:
Project supported by the Fund of Liaoning Provincial Department of Education (No. 2008349).

Twenty-one new derivatives have been synthesized using 3-substituted-4-amino-5-mercapto-1,2,4-triazale and pyrazole carboxylic acid as the staring materials. The structures of the title compounds were characterized by IR, ¹H NMR and elemental analyses. The wheat gemma method preliminary bioassay results indicated that some compounds display herbicidal activity to some extent, and bacteriostatic activity test results show that the part of compounds show excellent fungicidal activity, particularly compounds 3g and 3h exhibit higher than the others, and were similar with chloramphenicol. The minimum inhibitory concentrations (MIC) of 3g and 3h with Escherichia coli and Staphylococcus aureus is 6.25 and 3.13 mg/L, and 12.5 and 6.25 mg/L, respectively.

Key words: 1,2,4-triazolo[3,4-b]benzothiazole, synthesis, biological activity

Cite this article

Yao Mingxing, An Yue, Yan Jie, Tian Xing, Wei Shi. Synthesis and Biological Activities of Novel Substituted-pyrazole 1,2,4-Triazolo[3,4-b]benzothiazole[J]. Chin. J. Org. Chem., 2013, 33(05): 1015-1021.

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含吡唑取代基的1,2,4-三唑[3,4-b]-1,3,4-噻二唑类衍生物的合成及生物活性

Synthesis and Biological Activities of Novel Substituted-pyrazole 1,2,4-Triazolo[3,4-b]benzothiazole

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