5-氨基-4-甲基噻唑-2-甲酰芳胺类化合物的合成及其生物活性
收稿日期: 2017-05-19
修回日期: 2017-07-03
网络出版日期: 2017-08-09
基金资助
湖南省自然科学基金（No.2016JJ5019）资助项目.
Synthesis and Biological Activity of 5-Amino-4-methyl-N-phenylthiazole-2-carboxamide
Received date: 2017-05-19
Revised date: 2017-07-03
Online published: 2017-08-09
Supported by
Project supported by the Hunan Provincial Natural Science Foundation (No. 2016JJ5019).
曹蕾 , 孙景伟 , 刘强 , 钱程 , 杜彦林 , 许望津 , 陈开义 , 刘建兵 . 5-氨基-4-甲基噻唑-2-甲酰芳胺类化合物的合成及其生物活性[J]. 有机化学, 2017 , 37(11) : 3031 -3036 . DOI: 10.6023/cjoc201705029
Using seedvax as leading compound, seventeen new seedvax analogues N-substituted-4-methyl-5-aminothia-zole-2-benzamides were designed and synthesized. The structures of the target compounds were characterized by 1H NMR, 13C NMR, HRMS and IR spectral analyses. The preliminary bioassay results of fungicidal activities (FA) in vitro showed that most of the target compounds displayed higher activities than seedvax. Among them, the FA against Alternaria solani of one compound is 2.6 times of seedvax, the FA of 6 compounds against cucumber Fusarium wilt are more than 2 times of that of seedvax; the FA of 16 compounds against Colletotrichun orbiculare and Fusarium fujikuroi were higher than that of positive control. Especially, the FA against Colletotrichun orbiculare of seven compounds are more than twice of seedvax.
Key words： 5-aminothiazole; benzamide; synthesis; biological activity
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