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Antibacterial, antifungal and antileishmanial activities of indolone-N-oxide derivatives

Ibrahim, Hany and Furiga, Aurélie and Najahi, Ennaji and Pigasse Hénocq, Christel and Nallet, Jean-Pierre and Roques, Christine and Aubouy, Agnes and Sauvain, Michel and Constant, Patricia and Daffé, Mamadou and Nepveu, Françoise Antibacterial, antifungal and antileishmanial activities of indolone-N-oxide derivatives. (2012) The Journal of Antibiotics, vol. 65 (n° 10). pp 499-504. ISSN 0021-8820 (Unpublished)

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Official URL: http://dx.doi.org/10.1038/ja.2012.60

Abstract

An alarming increase in microbial resistance to traditional drugs and classical pharmacophores has spurred the search for new antimicrobial compounds. Indolone-N-oxides (INODs) possess a redox pharmacophore with promising, recently established, antimalarial activities. In this study, the anti-infectious properties of a series of INODs were investigated. The antibacterial activity was evaluated against five bacterial strains Gram-positive (Staphylococcus aureus, Enterococcus hirae), Gram-negative (Pseudomonas aeruginosa, Escherichia coli) and acid-fast (Mycobacterium tuberculosis). The antifungal activity was assessed using two fungal strains (Aspergillus niger, Candida albicans). The antileishmanial activity was tested against two leishmanial strains, axenically-cultured amastigote (Leishmania infantum, Leishmania amazonensis). The pharmacological activities are discussed as a function of structural and lipophilic characteristics. The Gram-positive bacterial strain E. hirae was found to be the most sensitive strain, whereas the Gram-negative E. coli was resistant to this family of compounds. One compound (64) was more potent than nalidixic acid against E. hirae, whereas another one (52) was equipotent as clotrimazole against C. albicans. INODs were microbe -cidal rather than -static. INODs showed good antitubercular activity in the low micromolar range (similar to ciprofloxacin). In addition, INOD-antiprotozoal potencies were confirmed against the leishmania parasite. INODs showed a broad spectrum of antimicrobial activity and offer a promising anti-infectious prototype worthy of being developed.

Item Type:Article
Additional Information:Uncorrected proof
Audience (journal):International peer-reviewed journal
Uncontrolled Keywords:
Institution:French research institutions > Centre National de la Recherche Scientifique - CNRS (FRANCE)
Université de Toulouse > Institut National Polytechnique de Toulouse - INPT (FRANCE)
French research institutions > Institut de Recherche pour le Développement - IRD (FRANCE)
Université de Toulouse > Université Paul Sabatier-Toulouse III - UPS (FRANCE)
Other partners > IDEALP'PHARMA (FRANCE)
Other partners > Universidad Peruana Cayetana Heredia - UPCH (PERU)
Other partners > Université de Sfax (TUNISIA)
Laboratory name:
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Deposited By: Vincent GERBAUD
Deposited On:16 Apr 2014 07:26

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