新型1,3,4-噁二唑类化合物的设计、合成及杀细菌活性

Design,synthesis and bactericidal activity of novel 1,3,4-oxadiazole compounds

[目的]发现结构新颖的高效杀细菌剂。[方法]以取代苯甲酸为起始原料,采用活性亚结构拼接策略。[结果]设计、合成了一系列1,3,4-噁二唑类化合物,其结构经1H NMR和ESI-MS确证。初步的温室生物活性测试结果表明,化合物7d具有优异的杀细菌活性,在测试质量浓度为400 mg/L时,化合物7d对甜瓜果斑病的防效高达91.71%,优于对照药剂硫酸链霉素。[结论]化合物7d可作为先导化合物进行进一步研究。

[Aims]In order to discover novel bactericides with more effective activity.[Methods]A series of 1,3,4-oxadiazole compounds were designed and synthesized on the principle of biologically active factor splicing using substituted benzoic acid as the starting material.[Results]The structures were confirmed by~1H NMR and ESI-MS.The preliminary bioassay results in greenhouse showed that compound 7d had excellent bactericidal activity.At the test concentration of 400 mg/L,the control effect of compound 7d on bacterial fruit blotch was as high as 91.71%,which was better than that of the control agent streptomycin sulfate.[Conclusions]Compound 7d can be further studied as a lead compound.