ANTIMICROBIAL ACTIVITY OF 9-OXO AND 9-THIO ACRIDINES - CORRELATION WITH INTERCALATION INTO DNA AND EFFECTS ON MACROMOLECULAR BIOSYNTHESIS

被引：23

作者：

CREMIEUX, A

CHEVALIER, J

SHARPLES, D

BERNY, H

GALY, AM

BROUANT, P

GALY, JP

BARBE, J

机构：

[1] FAC PHARM MARSEILLE, GERCTOP, CNRS, URA 1411, F-13385 MARSEILLE 5, FRANCE

[2] UNIV MANCHESTER, DEPT PHARM, MANCHESTER M13 9PL, LANCS, ENGLAND

来源：

RESEARCH IN MICROBIOLOGY | 1995年 / 146卷 / 01期

关键词：

CHEMOTHERAPY; ACRIDINE; DERIVATIVES; ANTIMICROBIAL ACTIVITY; INHIBITORY INDEXES; BACTERICIDAL INDEXES; ARN SYNTHESIS; INTERCALATION INTO DNA; GYRASE INHIBITION; MACROMOLECULAR SYNTHESIS;

D O I：

10.1016/0923-2508(96)80272-5

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

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.

引用

页码：73 / 83

页数：11

共 28 条

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