利用生物活性叠加原理,以4-氨基-5-甲基-1,2,4-三唑-3-硫酮为原料,设计合成了15个未见报道的化合物2-N-2′,3′,4′,6′-四-O-乙酰基-β-D-吡喃葡萄糖基-4-N-取代苯基亚胺基-5-甲基-1,2,4-三唑(2a～2e),4-N-取代苄基氨基-5-甲基-1,2,4-三唑(3a～3e)和2-N-2′,3′,4′,6′-四-O-乙酰基-β-D-吡喃葡萄糖基-4-N-取代苄基氨基-5-甲基-1,2,4-三唑(4a～4e).其结构经IR,1H NMR,13C NMR和元素分析确认.生物活性测试表明,所有化合物均表现出一定的抑菌活性,尤其是化合物4b对大肠杆菌和金黄色葡萄球菌的最小抑菌浓度为8μg/mL,明显优于市售抗菌药物氟康唑,表现出较强的抗细菌活性;同时,与三氯生相比,所有化合物对白色念珠菌的最小抑菌浓度(MIC)均小于或等于32μg/mL,亦表现出较好的抗真菌活性. Using the principle of bioactivity stacking and using 4-amino-5-methyl-1,2,4-triazole-3-thione as raw materials, 15 unreported compounds 2-N-2 ’, 3 ’, 4’, 6’-tetra-O-acetyl-β-D-glucopyranosyl-4-N-substituted phenylimino-5-methyl-1,2,4-triazole ~ 2e), 4-N-substituted benzylamino-5-methyl-1,2,4-triazole (3a ~ 3e) and 2-N-2 ’, 3’, 4 ’, 6’- O-acetyl-β-D-glucopyranosyl-4-N-substituted benzylamino-5-methyl-1,2,4-triazole (4a ~ 4e) 13C NMR and elemental analysis confirmed that all compounds showed some antibacterial activity, in particular, the minimum inhibitory concentration of 4b on Escherichia coli and Staphylococcus aureus was 8μg / mL, significantly better than the commercially available The antibacterial drug fluconazole showed a strong antibacterial activity. Meanwhile, all compounds showed a minimum inhibitory concentration (MIC) of less than or equal to 32 μg / mL against Candida albicans compared with triclosan, Good antifungal activity.