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新型1,2,3-三唑类化合物的合成及抗菌构效关系

彭春勇 卢俊瑞 辛春伟 李建发 戢丹 鲍秀荣

高等学校化学学报2013,Vol.34Issue(6):1394-1402,9.
高等学校化学学报2013,Vol.34Issue(6):1394-1402,9.DOI:10.7503/cjcu20121063

新型1,2,3-三唑类化合物的合成及抗菌构效关系

Synthesis and Antibacterial Structure-activity Relationship of Novel 1,2,3-Triazoles

彭春勇 1卢俊瑞 1辛春伟 1李建发 1戢丹 1鲍秀荣1

作者信息

  • 1. 天津理工大学化学化工学院,天津300384
  • 折叠

摘要

Abstract

According to active groups combination principle,seventeen compounds 1-(4-substituted phenyl)-5-substituted phenylbutyronitrile-4-substituted 1,2,3-triazoles (7a-7c,13a-13d) and 1-(4-substituted phenyl)-5-substituted benzylamino-4-substituted 1,2,3-triazoles(5a-Sc,10a-10c and 14a-14d) were designed and synthesized through diazotization,cyclization and condensation reactions from 4-substituted aniline,while compounds 5a-5c,7b,7c,10a,10c,13b-13d and 14b-14d have never been reported.Their structures were confirmed by IR,1H NMR and 13C NMR.The preliminary bioassay showed that all target compounds possessed efficient antibacterial activities,especially,they all exhibited better activities against Escheri-chia coli than fluconazole,while against Staphylococcus aureus,compounds 7a and 10c were more effective than fluconazole,and compounds 13a and 13c were as good as triclosan against Monilia albican.

关键词

1,2,3-三唑/席夫碱/抗菌/构效关系

Key words

1,2,3-Triazole/ Shift base / Antibacterial/ Structure-activity relationship

分类

化学化工

引用本文复制引用

彭春勇,卢俊瑞,辛春伟,李建发,戢丹,鲍秀荣..新型1,2,3-三唑类化合物的合成及抗菌构效关系[J].高等学校化学学报,2013,34(6):1394-1402,9.

基金项目

国家自然科学基金(批准号:20976135,21176194)资助. (批准号:20976135,21176194)

高等学校化学学报

OA北大核心CSCDCSTPCD

0251-0790

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