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Ibrahim H., Furiga A., Najahi E., Henocq C. P., Nallet J. P., Roques C., Aubouy Agnès, Sauvain Michel, Constant P., Daffe M., Nepveu Françoise. (2012). Antibacterial, antifungal and antileishmanial activities of indolone-N-oxide derivatives. Journal of Antibiotics, 65 (10), p. 499-504. ISSN 0021-8820.

Titre du document
Antibacterial, antifungal and antileishmanial activities of indolone-N-oxide derivatives
Année de publication
2012
Type de document
Article référencé dans le Web of Science WOS:000310564800003
Auteurs
Ibrahim H., Furiga A., Najahi E., Henocq C. P., Nallet J. P., Roques C., Aubouy Agnès, Sauvain Michel, Constant P., Daffe M., Nepveu Françoise
Source
Journal of Antibiotics, 2012, 65 (10), p. 499-504 ISSN 0021-8820
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.
Plan de classement
Santé : généralités [050] ; Entomologie médicale / Parasitologie / Virologie [052]
Identifiant IRD
PAR00009521
 DOI
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