Universidad Peruana Cayetano Heredia

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

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dc.contributor.author Ibrahim, H.
dc.contributor.author Furiga, A.
dc.contributor.author Najahi, E.
dc.contributor.author Pigasse Hénocq, C.
dc.contributor.author Nallet, J.-P.
dc.contributor.author Roques, C.
dc.contributor.author Aubouy, A.
dc.contributor.author Sauvain, Michel Henri Auguste
dc.contributor.author Constant, P.
dc.contributor.author Daffé, M.
dc.contributor.author Nepveu, F.
dc.date.accessioned 2022-01-18T19:26:49Z
dc.date.available 2022-01-18T19:26:49Z
dc.date.issued 2012
dc.identifier.uri https://hdl.handle.net/20.500.12866/10915
dc.description.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. en_US
dc.language.iso eng
dc.publisher Springer
dc.relation.ispartofseries Journal of Antibiotics
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
dc.subject Controlled Study en_US
dc.subject Animal Cell|Unclassified Drug en_US
dc.subject Mycobacterium Tuberculosis en_US
dc.subject Bacterium Culture en_US
dc.subject Anti-Bacterial Agents en_US
dc.subject Leishmania en_US
dc.subject Bacteria (Microorganisms) en_US
dc.subject Escherichia Coli en_US
dc.subject Ciprofloxacin en_US
dc.subject Bacterial Growth en_US
dc.subject Antibiotic Sensitivity en_US
dc.subject Nalidixic Acid en_US
dc.subject Antifungal Agents en_US
dc.subject Candida Albicans en_US
dc.subject Minimum Inhibitory Concentration en_US
dc.subject Antifungal Agent en_US
dc.subject Bacterial Strain en_US
dc.subject Negibacteria en_US
dc.subject Gram Negative Bacterium en_US
dc.subject Structure Activity Relation en_US
dc.subject Structure-Activity Relationship en_US
dc.subject Cytotoxicity en_US
dc.subject Antibacterial Activity en_US
dc.subject Antiprotozoal Activity en_US
dc.subject Indoles en_US
dc.subject Indolone N Oxide Derivative en_US
dc.subject Microbial Viability en_US
dc.subject Oxides en_US
dc.subject Pharmacodynamics en_US
dc.subject Posibacteria en_US
dc.subject Redox Pharmacophore en_US
dc.title Antibacterial, antifungal and antileishmanial activities of indolone-N-oxide derivatives en_US
dc.type info:eu-repo/semantics/article
dc.identifier.doi https://doi.org/10.1038/ja.2012.60
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#3.01.05
dc.relation.issn 1881-1469


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