摘要
目的合成3-三氟甲基-4-氨基-5-巯基-1,2,4-三唑衍生物并对其进行抗真菌活性研究。方法以3-三氟甲基-4-氨基-5-巯基-1,2,4-三唑(Ⅰ)为起始原料,与卤苄在无水乙醇中回流制得中间体3-三氟甲基-4-氨基-5-(取代)苄硫基-1,2,4-三唑(Ⅱ),Ⅱ与2,4-二氯苯甲醛反应得目标物3-三氟甲基-5-(取代)苄硫基-1,2,4-三唑希夫碱Sch iff,s(Ⅲ)。对中间体Ⅰ、Ⅱ和目标物Ⅲ进行了体外抑菌活性测试。结果合成了9个新的目标物Ⅲ,用1H-NMR和元素分析确定了中间体Ⅱ和目标物Ⅲ的结构。初步体外抑菌实验表明:3-三氟甲基-4-氨基-5-巯基-1,2,4-三唑衍生物对常见深部致病真菌有一定的体外抑制活性,但均弱于对照品氟康唑、特比萘芬和伊曲康唑。结论合成的目标物Ⅲ衍生物对常见深部致病真菌有一定的活性,对浅部真菌的活性有待进一步研究。
OBJECTIVE Synthesis 3-trifluoromethyl-4-amino-5-mercapto-1,2,4-triazole derivatives and put up the study of antifungal activity. METHODS The target compounds Ⅲ were synthesized by the condensation between 2,4-dichlorobenzaldehyde and the intermediates （ Ⅱ ） 3-trifluoromethyl-4-amino-5-benzylsulfide-1,2,4-triazole which were produced from a reaction of the starting material 3-trifluoromethyl-4-amino-5-mercapto-1,2,4-triazole and benzyl halide in an alcoholic medium. RESULTS Synthesis 9 new target compounds III, all intermediates Ⅱ and target compounds Ⅲ were confirmed by ^1HNMR and elemental analysis. Results of preliminary biological tests showed 3-trifluoromethyl-4-amino-5-mercapto-1,2,4-triazole derivatives exhibited activity against deep fungal to some extent, but the antifungal activities were ovbious lower than fluconazole,terbinafine and Itraconazole. CONCLUSION Synthesis of target compounds Ⅲ derivatives exhibited activity against deep fungal to some extent, but their activities against superficial fungal should do further study.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2007年第2期122-125,共4页
Chinese Journal of Modern Applied Pharmacy
