取代二噁二唑硫醚及砜衍生物合成及抗菌活性

Synthesis and Antibacterial Activity of Bisoxadiazole Sulfurether/Sulfone Derivatives

20种二唑硫醚 (3a～ 3j)及砜 (4a～ 4 j)衍生物通过二唑巯醇 (2a～ 2j)与二唑氯甲烷 (1)缩合及氧化被合成 ,结构由IR、1HNMR、MS和元素分析确证。体外抗活性结果表明 ,在质量分数 0 0 1%的浓度下 ,硫醚衍生物 3b对金黄色葡萄球菌、3h对变形杆菌表现较强的抑制活性 ,而砜衍生物 4b、4c、4d和 4f对大肠杆菌表现较强的抑制活性 。

Twenty 1,3,4-oxadiazole sulfurethers(3a～3j) and corresponding sulfone derivatives(4a～4j) were synthesized via condensation of 1,3,4-oxadiazole chloromethane(1) with the corresponding 1,3,4-oxadiazole thiols(2a～2j) followed by oxidation with 30% H 2O 2 in the presence of catalyst Na 2WO 4, and their structures were confirmed by IR, 1HNMR, MS and elemental analysis. Among the compounds synthesized, the sulfurether compounds (3b) and (3h) exhibited considerably strong inhibiting activity to Staphylococcus aureus and Proteus vulgaris in dosage of 1.0×10 -4(mass fraction), the sulfone compounds 4b, 4c, 4d and 4f exhibited mediumly inhibiting activity to Escherichia.coli, whereas the other compounds showed weak or even no antibacterial activity.