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苯基杂环的酰胺的合成及其构效关系研究【字数:6671】

2024-11-03 13:25编辑: www.jxszl.com景先生毕设

目录
摘要Ⅲ
关键词Ⅲ
AbstractⅣ
引言
引言1
1实验设计 1
2实验材料和方法 2
2.1仪器与材料 2
2.2合成方法 2
2.2.1含不同取代基的4苯基噻唑2羧酸(Ac1)的合成2
2.2.2含不同取代基的1苯基5甲基1H吡唑3羧酸的合成3
2.2.3 5(2氯苯基)1,3,4噻二唑2羧酸的合成3
2.2.4 5(2氯苯基)1,3,4噁二唑2羧酸的合成4
2.2.5 6(2氯苯基)烟酸的合成4
2.2.6含不同取代基的联苯胺的合成4
2.2.7 A系列化合物的合成5
2.2.8含不同取代基的噁二唑苯胺的合成 6
2.2.9 B系列化合物的合成7
2.2.10含不同取代基的苯基噁二唑胺的合成7
2.2.11 C 系列化合物的合成8
2.3 结构鉴定方法8
2.4 抗真菌活性测定方法8
3结果与分析9
3.1化合物的物理参数与波谱数据9
3.2化合物波谱分析15
3.3化合物抗真菌活性分析15
4讨论17
致谢18
参考文献19
苯基杂环的酰胺的合成及其构效关系研究
摘 要
杂环化合物及其衍生物被报道具有广泛的生物活性,含有杂环的化合物可表现出良好的杀菌性能。杂环化合物,尤其是含氮杂环化合物因为具有类似生物体内生物碱的结构,对靶标具有高度的专一性,并且有优秀的环境相容性,常用于农药结构的设计之中。此类农药常具有广泛的抗菌活性,目前已成为农药创制的热点之一。噻唑、吡唑、噁二唑、噻二唑以及吡啶都属于含氮杂环,其衍生物已被广泛报道具有潜在的杀菌活性。本文以广泛使用的商品化农药啶酰菌胺为先导化合物,将五种含氮杂环引入先导化合物结构,平板抑菌活性结果显示噁二唑酰胺衍生物具有一定的抑菌活性,选择噁二唑杂环进行进一步的结构衍生,又将噁二唑杂环引入啶酰菌胺氨基侧,共得到3个系列共35个化合物,并测试了这些化合 *51今日免费论文网|www.51jrft.com +Q: ¥351916072
物对常见的四种植物病原真菌的抑制活性。
SYNTHESIS AND STRUCTUREACTIVITY RELATIONSHIP OF PHENYL HETEROCYCLIC AMIDES
ABSTRACT
Heterocyclic compounds and their derivatives have been reported to have high biological activities. They show good bactericidal properties. Heterocyclic compounds, especially nitrogencontaining heterocyclic compounds, are often used in the design of pesticide structures because of their specificity to targets and excellent environmental compatibility due to the similarity structure of alkaloids in organisms. These pesticides often have a wide range of antibacterial activities, and have become one of the hotspots in the development of pesticides. Thiazole, pyrazole, oxadiazole, thiadiazole and pyridine are all nitrogencontaining heterocycles, and their derivatives have been reported to have potential bactericidal activity. In this paper, five nitrogencontaining heterocycles were introduced into the structure of the lead compounds, the results of plate antibacterial activity showed that oxadiazole amide derivatives had a certain antibacterial activity. Oxadiazole heterocycles were selected for further structural derivation.  In addition, oxadiazole heterocycle was introduced into the amino side of boscalid. These series of 35 compounds were designed and synthesized, and the inhibitory activities of these compounds against six common plant pathogenic fungi were tested.

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