新结构硫脲类化合物的合成、鉴定及抑菌活性评价

Synthesis, characterizations and antimicrobial activities of new thiourea derivatives

摘要:

【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。

关键词:硫脲衍生物，异硫氰酸酯，抗菌，新型隐球菌

Abstract:

[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.

Key words:Thiourea derivatives, Isothiocyanate, Antibacterial, Cryptococcus neoformans