Abstract
The dramatic worldwide increase of dangerous infections by resistant and multi-resistant microbes makes the search of new molecules and new chemical entities an important topic in Medicinal Chemistry. As the ideal drug candidate has not been attained, an intensive search for new and innovative antimicrobials is still needed. A small series of 3- amino/nitrocoumarins without substitutions or substituted by methyl or methoxy groups at different positions were synthesized and evaluated for their antibacterial and antifungal activities against clinical isolates of Staphylococcus aureus, Escherichia coli and Candida albicans strains. Some of these structurally simple molecules exhibited antibacterial activity. The preliminary SAR study showed that the antibacterial activity against E. coli and S. aureus was dependent on the kind and position of the substitution pattern at the coumarin moiety.
Keywords: Aminocoumarins, nitrocoumarins, coumarin synthesis, antibacterial assays, inhibition zones, minimum inhibitory concentrations, S. aureus, E. coli
Medicinal Chemistry
Title:Looking for New Targets: Simple Coumarins as Antibacterial Agents
Volume: 8 Issue: 6
Author(s): Maria Joao Matos, Saleta Vazquez-Rodriguez, Lourdes Santana, Eugenio Uriarte, Cristina Fuentes-Edfuf, Ysabel Santos and Angeles Munoz-Crego
Affiliation:
Keywords: Aminocoumarins, nitrocoumarins, coumarin synthesis, antibacterial assays, inhibition zones, minimum inhibitory concentrations, S. aureus, E. coli
Abstract: The dramatic worldwide increase of dangerous infections by resistant and multi-resistant microbes makes the search of new molecules and new chemical entities an important topic in Medicinal Chemistry. As the ideal drug candidate has not been attained, an intensive search for new and innovative antimicrobials is still needed. A small series of 3- amino/nitrocoumarins without substitutions or substituted by methyl or methoxy groups at different positions were synthesized and evaluated for their antibacterial and antifungal activities against clinical isolates of Staphylococcus aureus, Escherichia coli and Candida albicans strains. Some of these structurally simple molecules exhibited antibacterial activity. The preliminary SAR study showed that the antibacterial activity against E. coli and S. aureus was dependent on the kind and position of the substitution pattern at the coumarin moiety.
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Cite this article as:
Joao Matos Maria, Vazquez-Rodriguez Saleta, Santana Lourdes, Uriarte Eugenio, Fuentes-Edfuf Cristina, Santos Ysabel and Munoz-Crego Angeles, Looking for New Targets: Simple Coumarins as Antibacterial Agents, Medicinal Chemistry 2012; 8 (6) . https://dx.doi.org/10.2174/1573406411208061140
DOI https://dx.doi.org/10.2174/1573406411208061140 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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