苯联三唑(磺)酰胺衍生物的合成及抑菌活性  

Synthesis and antifungal activity of phenyltriazole derivatives with sulfonamide or amide groups

作　　者：徐成硕 王传平 王红梅 尹培军 秦启学 郝双红[1] XU Cheng-shuo;WANG Chuan-ping;WANG Hong-mei;YIN Pei-jun;QIN Qi-xue;HAO Shuang-hong(Research Center of Bio-pesticides Engineering&Tech of Shandong Province,College of Chemistry&Pharm,Qingdao Agricultural University,Qingdao 266109,Shangdong,China;Technology Center of Qingdao Customs District,Qingdao 266109,Shangdong,China)

机构地区：[1]青岛农业大学化学与药学院,山东省生物农药工程技术研究中心,山东青岛266109 [2]青岛海关技术中心,山东青岛266109

出　　处：《农药》2023年第1期13-16,共4页Agrochemicals

基　　金：2021年山东省大学生创新创业训练计划项目(S202110435116)。

摘　　要：[目的]寻找新杀菌活性的苯联三唑(磺)酰胺衍生物。[方法]设计合成了系列N-(4-(3-苯基-1H-1,2,4-三唑-1-基)苯基)苯磺酰胺或苯甲酰胺衍生物,以菌丝生长速率法对其抑菌活性进行了初步评价。[结果]合成了3类12个N-(4-(3-苯基-1H-1,2,4-三唑-1-基)苯基)苯磺酰胺或苯甲酰胺衍生物,结构经1H及13C NMR确证。[结论]目标化合物收率为60.7%~81.3%;该类化合物对番茄灰霉病菌有较强抑制作用,其中11个化合物的抑菌率均大于85%,优于对照药剂烯唑醇(80.8%);5个化合物对苹果腐烂病菌的抑菌率大于74%,优于烯唑醇(68.6%)。[Aims]This study aims to search for new antifungal phenyltriazoles with sulfonamide or amide groups.[Methods]A series of N-(4-(3-phenyl-1H-1,2,4-triazol-1-yl)phenyl)benzenesulfonamide or benzamide derivatives were designed and synthesized.Their antifungal activities against the mycelia growth of 5 fungi were examined.[Results]12 N-(4-(3-Phenyl-1H-1,2,4-triazol-1-yl)phenyl)benzenesulfonamideorbenzamidederivativesweresynthesized,theirstructures were confirmed by 1H and 13C NMR.[Conclusions]The yields of target compounds were in the range of 61.7%-81.3%.These compounds showed certain antifungal activities against the phytopathogens tested.11 Of them exhibited higher inhibition activity with>85%control against Botrytis cinerea than commercial fungicide diniconazole(80.8%).5 Compounds exhibited higher inhibition with>74%control against Valsa mali than diniconazole(68.6%).

关 键 词：3-苯基-1H-1 2 4-三唑 磺酰胺 酰胺 合成 抑菌活性 

分 类 号：TQ460.3[化学工程—制药化工]