邢程远,黄华,杨鹏辉,姜林.化学通报,2017,80(9):868-872. |
含吡啶环的N-(1,3,4-噻二唑-2-基)苯甲酰胺类化合物的合成及其抑菌活性 |
Synthesis and Antifungal Activity of N-(1,3,4-thiadiazol-2-yl)benzamide Compounds Bearing Pyridine Moiety |
投稿时间:2017-02-13 修订日期:2017-03-24 |
DOI: |
中文关键词: 吡啶 噻二唑 酰胺 合成 抑菌活性 |
英文关键词:pyridine, thiadiazole, amide, synthesis, antifungal activity |
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中文摘要: |
以3-吡啶乙酸盐酸盐与氨基硫脲为原料经环化反应制备中间体2-氨基-5-(3-吡啶亚甲基)-1,3,4-噻二唑,后者与取代苯甲酰氯反应合成了一系列含吡啶环的N-(1,3,4-噻二唑-2-基)取代苯甲酰胺3a ~ 3k,其结构通过IR, 1H NMR,13C NMR和元素分析确证。用菌丝生长速率法测定了目标化合物对灰霉菌的离体抑菌活性,结果表明,部分化合物对病原菌有一定的抑制活性。 |
英文摘要: |
The intermediate 2-amino-5-(3-pyridinylmethyl)-1,3,4-thiadiazole was prepared from 3-pyridinylacetic acid hydrochloride and thiosemicarbazide by cyclization, followed by reaction with substituted benzoyl chloride to yield the target compound, N-[5-(3-pyridylmethyl)-1,3,4-thiadiazol-2-yl]benzamide (3a ~ 3k). Their structures were elucidated by IR, 1H NMR, 13C NMR and elemental analysis. Meanwhile, the target compounds were evaluated for their antifungal activities against B. cinerea by the mycelium growth rate method, and the results indicated that some compounds displayed antifungal activity to some extent. |
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