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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 被引量:2

Synthesis and Biological Activity of 5-Amino-4-methyl-Nphenylthiazole-2-carboxamide
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摘要 以拌种灵结构为先导,设计并合成了17个5-氨基-4-甲基噻唑-2-甲酰芳胺拌种灵类似物,其结构均经1H NMR,13C NMR,HRMS及IR确证.初步离体生物活性测试结果表明,大多目标化合物的杀菌活性高于对照物拌种灵.其中1个化合物对番茄早疫的杀菌活性是对照样拌种灵的2.6倍;5个化合物对黄瓜枯萎的杀菌活性是拌种灵的2倍以上.16个化合物对西瓜炭疽和水稻恶苗的杀菌活性均高于阳性对照,其中7个化合物对西瓜炭疽的杀菌活性高于阳性对照一倍以上. Using seedvax as leading compound,seventeen new seedvax analogues N-substituted-4-methyl-5-aminothiazole-2-benzamides were designed and synthesized.The structures of the target compounds were characterized by 1 H NMR,13 C 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.
出处 《有机化学》 SCIE CAS CSCD 北大核心 2017年第11期3031-3036,共6页 Chinese Journal of Organic Chemistry
基金 湖南省自然科学基金(No.2016JJ5019)资助项目~~
关键词 5-氨基噻唑 苯甲酰胺 合成 生物活性 5-aminothiazole benzamide synthesis biological activity
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