ANTIMICROBIAL ACTIVITY OF 9-OXO AND 9-THIO ACRIDINES - CORRELATION WITH INTERCALATION INTO DNA AND EFFECTS ON MACROMOLECULAR BIOSYNTHESIS
ANTIMICROBIAL ACTIVITY OF 9-OXO AND 9-THIO ACRIDINES - CORRELATION WITH INTERCALATION INTO DNA AND EFFECTS ON MACROMOLECULAR BIOSYNTHESIS
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DOI：
10.1016/0923-2508(96)80272-5
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发表时间：
1995-01-01
影响因子：
2.6
通讯作者：
BARBE, J
中科院分区：
文献类型：
--
作者：
CREMIEUX, A;CHEVALIER, J;BARBE, J
研究了几种新的9-吖啶酮和9-硫代烷基吖啶类化合物对大肠杆菌、金黄色葡萄球菌、耻垢分枝杆菌和白色念珠菌的抗菌活性。使用微孔板测定法测定最小抑菌、杀菌和杀真菌浓度，该测定法能够计算抑菌、杀菌和杀真菌指数。这些指标有利于结构/活性关系的研究。DNA嵌入能力和DNA超螺旋抑制作用以及对大分子合成的抑制作用进行了测定。结果表明，插入DNA，这是通常假设的吖啶的作用机制，不能与性能检查。然而，RNA合成的抑制可能涉及药物的抗微生物活性。
The antimicrobial activity of several new 9-acridinones and 9-thioalkylacridines towards Escherichia coli, Staphylococcus aureus, Mycobacterium smegmatis and Candida albicans was investigated. Minimal inhibitory, bactericidal and fungicidal concentrations were determined using a microplate assay which enabled inhibitory, bactericidal and fungicidal indices to be calculated. These indices facilitated structure/activity relationship studies. DNA-intercalating capability and DNA supercoiling inhibitory effects as well as inhibitory effects on macromolecular synthesis were determined. Results showed that intercalation into DNA, which is the mechanism of action usually postulated for acridines, cannot be correlated with the properties examined. However, inhibition of RNA synthesis may be involved in the antimicrobial activity of the drugs.