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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。
Aim To synthesize 3-trifluoromethyl-4-amino-5-mercapto-1,2,4-triazole derivatives and study their antifungal activity. Methods 3-Trifluoromethyl-4-amino-5-mercapto-1,2,4-triazole (Ⅰ) was used as the starting material and refluxed with benzyl alcohol in absolute ethanol to obtain the intermediate 3- Methyl 4-amino-5- (substituted) benzylthio-1,2,4-triazole (Ⅱ) and Ⅱ were reacted with 2,4-dichlorobenzaldehyde to obtain the target 3-trifluoromethyl- - (substituted) benzylthio-1,2,4-triazole Schiff base Schiff, s (Ⅲ). The antibacterial activities of intermediates I, II and III were tested in vitro. Results Nine new target compounds were synthesized. The structures of intermediate Ⅱ and target Ⅲ were determined by 1H-NMR and elemental analysis. The preliminary in vitro bacteriostasis experiments showed that 3-trifluoromethyl-4-amino-5-mercapto-1,2,4-triazole derivatives had certain inhibitory activity in vitro against common pathogenic fungi, but both were weaker than the control Fluconazole, terbinafine and itraconazole. Conclusion The synthetic derivatives of Derivatives III have some activity on common pathogenic fungi, and the activity on superficial fungi needs to be further studied.