新型取代3-芳基-1,2,4-三唑并[3,4-b]苯并噻唑的合成及其杀菌活性  

Synthesis and Antifungal Activity of Novel Substituted3-aryl-1,2,4-triazolo[3,4-b]benzothiazoles

作　　者：翁建全[1] 黄华[1] 谭成侠[1] 刘幸海[1] 储为盛[1] 陈杰 

机构地区：[1]浙江工业大学化学工程与材料学院,杭州310032 [2]国家南方农药创制中心浙江基地生测部,杭州310023

出　　处：《有机化学》2012年第5期957-961,共5页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.30900959)资助项目~~

摘　　要：为了寻找新的含苯并噻唑稠杂环农药先导化合物,利用取代2-肼基苯并噻唑与取代苯甲酸在三氯氧磷中回流反应,合成了18个新型取代3-芳基-1,2,4-三唑并[3,4-b]苯并噻唑化合物,并利用1H NMR,EI-MS及元素分析对其结构进行了表征.初步生物活性试验结果表明,在50 mg/L浓度下,部分目标化合物对立枯丝核菌(Rhizoctonia solani)、西瓜壳二孢菌(Ascochyta citrullina)、香蕉枯萎病菌(Fusarium oxysporum f.sp.cubense)、烟草炭疽病菌(Colletotrichum nicotianae)具有中等杀菌活性.然而,部分化合物对灰葡萄孢菌(Botrytis cinerea)反而起到一定促进生长作用.In order to find new benzothiazole lead compounds, eighteen new substitued-3-aryl-l,2,4-triazolo[3,4-b]-benzo- thiazoles were synthesized by reacting substituted-2-hydrazinobenzothiazole with various substituted benzoic acids in POC13 under reflux condition. The structures of the title compounds were characterized by ~H NMR, EIMS techniques and elemental analysis. The preliminary bioassy results indicated that some of them showed moderate inhibition activity against Rhizoctonia solani, Ascochyta citrullina, Fusarium oxysporum f.sp. cubense and Colletotrichum nicotianae. Unexpectedly, some of them possessed certain promotion activity against Botrytis cinerea.

关 键 词：1 2 4-三唑并[3 4-b]苯并噻唑 合成 杀菌活性 

分 类 号：TQ455.4[化学工程—农药化工]