Antimicrobial activity of 9-oxo and 9-thio acridines: Correlation with intercalation into DNA and effects on macromolecular biosynthesis
| Autor: | A Crémieux, A.-M. Galy, Derek Sharples, J Chevalier, J. Barbe, J. P. Galy, H Berny, Pierre Brouant |
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| Rok vydání: | 1995 |
| Předmět: |
DNA
Bacterial Staphylococcus aureus In Vitro Techniques Microbiology Mycobacterium Structure-Activity Relationship Minimum inhibitory concentration chemistry.chemical_compound Bacterial Proteins Candida albicans Escherichia coli medicine Molecular Biology Antibacterial agent Dose-Response Relationship Drug biology Mycobacterium smegmatis General Medicine biology.organism_classification Antimicrobial RNA Bacterial Biochemistry chemistry Mechanism of action Acridines DNA supercoil medicine.symptom DNA |
| Zdroj: | Research in Microbiology. 146:73-83 |
| ISSN: | 0923-2508 |
| DOI: | 10.1016/0923-2508(96)80272-5 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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