Studies on 6-aminoquinolones: synthesis and antibacterial evaluation of 6-amino-8-methylquinolones.

doi:10.1021/JM950558V

Paper

Studies on 6-aminoquinolones: synthesis and antibacterial evaluation of 6-amino-8-methylquinolones.

Published Jan 19, 1996 · V. Cecchetti, A. Fravolini, M. Lorenzini

Journal of medicinal chemistry

55

Citations

2

Influential Citations

Full text

Abstract

The 6-aminoquinolone had previously been identified as a new class of quinolone antibacterial agents. To continue our structure-activity relationship (SAR) study in this series, novel 6-amino-8-methylquinolone derivatives have now been synthesized and evaluated for in vitro antibacterial activity. We have shown that the coupled presence of a methyl group at the C-8 position with an amino group at C-6 is effective for enhancing antibacterial activity, particularly against Gram-positive bacteria. The SARs associated with the N-1, C-6, and C-7 are discussed. The 1,2,3,4-tetrahydroisoquinolinyl derivative 19v showed the highest antibacterial activity with MIC values on Gram-positive bacteria superior to that of ciprofloxacin, especially against Staphylococcus aureus strains, including those strains which are methicillin-and ciprofloxacin-resistant.

In Vitro Study

Study Snapshot

6-amino-8-methylquinolone derivatives show enhanced antibacterial activity, particularly against Gram-positive bacteria, with 19v showing the highest activity against Staphylococcus aureus.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Studies on 6-aminoquinolones: synthesis and antibacterial evaluation of 6-amino-8-methylquinolones.

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