[目的]合成具有抗菌活性的新结构硫脲类化合物.[方法]通过α-异硫氰酸酯中间体与不同伯胺缩合合成硫脲类化合物,利用质谱、核磁分析鉴定结构,并评价其抑菌活性.[结果]合成了六种新结构的硫脲类化合物以及一种α-异硫氰酸酯类衍生物,对几种代表性病原细菌和真菌具有抑菌活性.其中,硫脲类化合物对新型隐球菌的抑制效果较为显著.[结论]通过不同结构硫脲类衍生物的合成,可能筛选出具有抑制新型隐球菌等致病菌的前体化合物.%[Objective] This study aimed to synthesize novel thiourea derivatives with good antimicrobial activities.[Methods] Thiourea derivatives were synthesized through condensation of various primary amines with the α-isothiocyanatoacrylic ester (ICE) intermediate;their structures were determined by MS and NMR analysis and their antimicrobial activities were then evaluated.[Results] Six novel thiourea derivatives and one new α-isothiocyanatoacrylic ester derivative were synthesized through condensation of corresponding primary amines with α-isothiocyanatoacrylic ester.The bioactivities of these compounds were tested against several representative pathogenic bacterium and fungus strains.Specifically,the thiourea derivatives showed considerable inhibition activities against Cryptococcus neoformans,the pathogen fungus of cryptococcosis.[Conclusion] Synthesis of new thiourea derivatives and test their biological activities is a potential way to discover small molecule drug leads.
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