新型桃金娘烯醛基双酰胺-噻二唑化合物的合成及其抗真菌活性

Chinese Journal of Synthetic Chemistry(2015)

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Abstract
以α-蒎烯为起始原料,经氧化制得桃金娘烯酸(3);脂肪族二酸在POC13作用下与氨基硫脲经脱水环合制得脂肪族双噻二唑(4a~4h);4a~4h分别与3经脱水反应合成了8个新型的桃金娘烯醛基双酰胺噻二唑化合物(5a~5h),其结构经1H NMR,13C NMR,IR和ESI-MS表征.抗真菌活性测试结果表明,在用药量为50μg·mL-1时,5a~5h对黄瓜枯萎病菌、花生褐斑病菌、苹果轮纹病菌、番茄早疫病菌和小麦赤霉病菌均有一定的抑制作用,其中桃金娘烯醛-辛二酸基双酰胺-噻二唑(5f)对苹果轮纹病菌的抑制率为60.3%,桃金娘烯醛-丁二酸基双酰胺-噻二唑(5b)和桃金娘烯醛-癸二酸基双酰胺-噻二唑(5h)对小麦赤霉病菌的抑制率分别为52.8%和54.4%.
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Key words
α-pinene,myrtenal,bisamide-thiadiazole,synthesis,antifungal activity
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