摘要：
将3-对氯苯基、3-对甲氧基苯基和3-正十一烷基-1,2,4-均三唑分别与5个芳香醛反应合成了15个Schiff碱,然后将Schiff碱、甲醛和吗啉进行多组分一锅反应,合成14个新型Mannich碱(PCTABM、PMTABM和PUTABM).为了对比探究3-取代基对分子生物活性的影响,以3-二茂铁基-1,2,4-均三唑为原料,利用相似的方法合成了4个3-二茂铁基-1,2,4-均三唑Mannich碱(FeTABM).应用IR,1H NMR和HRMS等对15种新物质进行了结构表征.评价了目标分子对植物生长调节活性、除草活性和抑制Cdc25B活性,结果发现,目标化合物在植物生长调节和除草活性中均表现出优良的活性,14个目标分子对Cdc25B表现出优良的抑制活性,其中7c、8e、9e、10b～10e的IC50值低于参照物Na3VO4,有望成为Cdc25B抑制剂.%15 Schiff bases were synthesized by the reactions of 3-p-chlorophenyl,3-p-methoxyphenyl and 3-n-pentyl-1,2,4-triazole with five different aromatic aldehydes,respectively.Then 14 novel Mannich bases (PCTABM,PMTABM and PETABM) were first afforded by the reactions of Schiff bases with formaldehyde and morpholine through multi-component one-pot reaction.In order to explore the effect of different 3-substituted groups on biological activities,four Mannich bases FcTABM of 3-ferrocenyl-1,2,4-triazole were also synthesized starting from 3-ferrocenyl-1,2,4-triazole by the similar method.IR,1H NMR and HRMS were used to characterize the structure of the target molecules.The biological activities of the target molecules were evaluated.As a result,the target compounds exhibited excellent activities in plant growth regulators and herbicidal activity.There are 14 target compounds exhibited excellent inhibitory activity against Cdc25B,in which the IC50 values of 7c,8e,9e,10b～10e IC50 were all smaller than the reference Na3VO4,which were expected to be Cdc25B inhibitors.
