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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Looking for New Targets: Simple Coumarins as Antibacterial Agents

Author(s): Maria Joao Matos, Saleta Vazquez-Rodriguez, Lourdes Santana, Eugenio Uriarte, Cristina Fuentes-Edfuf, Ysabel Santos and Angeles Munoz-Crego

Volume 8, Issue 6, 2012

Page: [1140 - 1145] Pages: 6

DOI: 10.2174/1573406411208061140

Price: $65

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


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