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利用生物活性亚结构拼接原理,将吡啶环、噻唑环引入到1,3,4-噁二唑母体结构中,设计并合成了一系列新型含吡啶(噻唑)的1,3,4-噁二唑衍生物.通过IR,1H NMR,EI-MS及元素分析等方法对所合成的化合物进行了结构表征.代表化合物2-(6-氯吡啶-3-甲硫基)-5-(吡啶-4-基)-1,3,4-噁二唑(I)经单晶X衍射证实了结构.初步测定了所合成化合物的杀菌活性,并比较了在1,3,4-噁二唑母体结构中引入噻唑杂环和引入吡啶杂环后其杀菌活性的差异.结果表明:目标化合物对测试的5种菌均具有一定的杀菌活性,对水稻纹枯病的抑制效果普遍优于对其它菌种的抑制效果;在1,3,4-噁二唑母体结构中引入噻唑杂环比引入吡啶杂环对其杀菌活性更有利.
Using the principle of bioactive sub-structure splicing, a series of novel 1,3,4-oxadiazoles containing pyridine (thiazole) were designed and synthesized by introducing the pyridine ring and thiazole ring into the 1,3,4-oxadiazole structure. The derivatives were characterized by means of IR, 1H NMR, EI-MS and elemental analysis. The representative compound 2- (6-chloropyridine-3-methylthio) -5- 4-yl) -1,3,4-oxadiazole (I) was confirmed by single-crystal X-ray diffraction. The bactericidal activities of the synthesized compounds were preliminarily determined. The results showed that the target compounds had certain bactericidal activities against five kinds of bacteria tested, and their inhibitory effects on sheath blight of rice were generally better than those of other bacteria The introduction of thiazole heterocycle into the 1,3,4-oxadiazole base structure was more favorable than the introduction of pyridine heterocycle for its bactericidal activity.