PMID: 7538688Jan 1, 1995Paper

Antimicrobial activity of 9-oxo and 9-thio acridines: correlation with interacalation into DNA and effects on macromolecular biosynthesis

Research in Microbiology
A CrémieuxJ Barbe

Abstract

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.

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Citations

Feb 18, 2011·Expert Opinion on Therapeutic Patents·Jatinder Kaur, Palwinder Singh
May 6, 2009·International Journal of Biological Macromolecules·Zuzana VantováJán Imrich
Apr 7, 2004·Médecine sciences : M/S·Jean-Marie Pagès

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