磺胺醌亚胺类化合物抑菌活性的测定

THE ANTIBACTERIAL ACTIVITY OF SULFONAMIDE-QUINONEIMINES

目的 :通过抗菌活性测定来探讨磺胺醌亚胺化合物的抗菌效力及其结构与活性间的关系 ,为新的抗菌药物研制提供依据。方法 :利用二倍稀释法测定了五种磺胺醌亚胺化合物对Staphylococcusaureus、Bacillussubtilis的最低抑菌浓度。结果 :磺胺醌亚胺类化合物具有很强的抑菌活性 ,大多较母体磺胺化合物强 ,其中磺胺醌亚胺对S .aureus和B .subtilis的抑菌活性分别为氨基苯磺胺的 2 .5和 1.2倍 ,磺胺嘧啶醌亚胺的抑菌活性分别为其母体化合物的 13.1和 6 .1倍 ,磺胺噻唑醌亚胺的抑菌活性为其母体化合物的 1.0 5和 6 5 .8倍 ,而磺胺吡啶醌亚胺对B .subtilis的抑菌活性有较大程度降低 ,仅为母体化合物的 6 .7%。结论 :磺胺醌亚胺化合物有比磺胺类药物更强的抗菌活性 。

OBJECTIVE:The antibacterial activity of sulfonamide quinoneimines(SQ) was studied in vitro in order to determine the potency of these antibacterial agents in solution and the relationship of the chemical structure and the antibacterial activity. METHODS: The antibacterial activity of 5 kinds SQ were tested with double dilution method on Staphalococcus aureus and Bacillus subtilis. RESULTS: Most of these derivatives have stronger activity than their precursor. The activity of sulfonilamide quinoneimine is 2.5 or 1.2 times as strong as sulfanilamide to S. aureus or B. subtilis. That of SQ is 13.1 or 6.1 times of the sulfadiarine, and SQ is 1.05 or 65.8 times of the sulfathiazole to S.aureus and B.subtilis. But that of sulfapyridine quinoneimine is only 6.7% of sulfapyridine to B. subtilis. CONCLUSION: With the chemical structure of sulfonamide changing to quinoneimine, the antibacterial activity of the SQ may be improved remarkably,or the antibacterial spectrum may be different.