Synthesis of Novel Amino/Nitro Substituted 3-Arylcoumarins as Antibacterial Agents

doi:10.3390/ECSOC-16-01036

Paper

Synthesis of Novel Amino/Nitro Substituted 3-Arylcoumarins as Antibacterial Agents

Published Oct 30, 2012 · M. Matos, S. Vazquez-Rodriguez, Cristina Fuentes-Edfuf

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Abstract

With the aim of exploring the antibacterial interest of the 3-arylcoumarinic skeleton, a new series of amino/nitro substituted 3-arylcoumarins was synthesized and evaluated for their antibacterial activity against clinical isolates Staphylococcus aureus (Gram-positive) and Escherichia coli (Gram-negative). This series was selected thinking on finding out the structural features for their antibacterial activity and selectivity. Therefore, in the present manuscript different positions of nitro, methyl, methoxy, amino and bromo substituents, under the 3-arylcoumarin scaffold, were reported. Some of these molecules exhibited antibacterial activity against S. aureus comparable to the standards – oxolinic acid and ampicillin. The best derivative of the studied series is compound 6, active and selective against S. aureus, with a MIC = 8 µg/mL. The preliminary structure-activity relationship (SAR) study showed that the antibacterial activity against S. aureus depends on the position of the substitution pattern on the 3-arylcoumarin moiety. Compound 6 will be the inspiration for the search of new active and selective antibacterial compounds.

In Vitro Study

Study Snapshot

Novel amino/nitro substituted 3-arylcoumarins show antibacterial activity and selectivity against Staphylococcus aureus, with compound 6 being the inspiration for the search of new active and selective compounds.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis of Novel Amino/Nitro Substituted 3-Arylcoumarins as Antibacterial Agents

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References

Citations

Synthetic Strategies and Biological Potential of Coumarin-Chalcone Hybrids: A New Dimension to Drug Design

Coumarin-chalcone hybrids show potential as effective biological scaffolds for drug discovery due to their diverse pharmacological activities and minimal side effects.