Synthesis and antileishmanial activity of 3-(alpha-azolylbenzyl)indoles.
J Enzyme Inhib Med Chem
; 17(6): 353-8, 2002 Dec.
Article
en En
| MEDLINE
| ID: mdl-12683669
ABSTRACT
The goal of the present study was to evaluate several azolyl-substituted indoles as new antileishmanial agents. Ten 3-(alpha-azolylbenzyl)indoles have been synthesized using Friedel-Crafts acylation as a key-step. All the target compounds were found to display high levels of activity when tested against Leishmania mexicana promastigotes in vitro. The most active compounds, showing an IC50 < 1 microM, were 5-bromo-1-ethyl-3-[(2,4-dichlorophenyl)(1H-imidazol-1-yl)methyl]-1H-indole 15 and its triazole analogue 17. Four representative compounds 15, 17, 22 and, 23 were also tested against intracellular amastigotes of L. mexicana using ketoconazole and meglumine antimoniate as reference compounds, the results of which are discussed.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Indoles
/
Antiprotozoarios
Límite:
Animals
Idioma:
En
Revista:
J Enzyme Inhib Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2002
Tipo del documento:
Article
País de afiliación:
Francia