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以取代1,2,3-噻二唑为原料,合成了一系列未见文献报道的含有1,2,3-噻二唑、1,2,4-三唑的双杂环类硫苷化合物(6a~6d)。目标化合物的结构经过1H NMR、13C NMR和IR等技术手段表征确认,重点对比了含西弗碱化合物5与还原后化合物6的抗菌活性变化。体外抑菌测试结果显示,所有化合物对大肠杆菌、金黄色葡萄球菌和白色念珠菌均表现出较好的抑制活性,含有西弗碱化合物5的抗菌活性普遍优于还原后化合物6,其中化合物5d表现出很强的抗菌活性,其最小抑菌浓度优于市售抗菌药氟康唑;所有目标化合物对白色念珠菌的最小抑菌浓度均小于或等于32 mg/L。
A series of bis-heterocyclic sulforaphane compounds containing 1,2,3-thiadiazole and 1,2,4-triazole have been synthesized by using 1,2,3-thiadiazole as starting material (6a to 6d). The structure of the target compound was confirmed by 1H NMR, 13C NMR and IR. The antibacterial activity of the target compound was compared with that of the reduced compound 6. In vitro antibacterial test results showed that all the compounds showed good inhibitory activity against Escherichia coli, Staphylococcus aureus and Candida albicans, and the antibacterial activity of the compound containing Sifuogen 5 was generally better than that of the reduced compound 6, in which compound 5d Showed a strong antibacterial activity, the minimum inhibitory concentration is better than the commercially available antibacterial fluconazole; all the target compounds against Candida albicans minimum inhibitory concentration of less than or equal to 32 mg / L.