1. Synthesis and Antileishmanial Activity of 3-(α-Azolylbenzyl)indoles.
- Author
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Marchand, Pascal, Le Borgne, Marc, Young Min Na, Fabrice, Pagniez, Hiam, Abdala, Guillaume, Le Baut, Patrice, and Le Pape, Patrice
- Subjects
LEISHMANIASIS treatment ,INDOLE ,LEISHMANIA ,PYRROLES ,AMASTIGOTES ,ACYLATION ,THERAPEUTICS - Abstract
The goal of the present study was to evaluate several azolyl-substituted indoles as new antileishmanial agents. Ten 3-(α-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 IC 50 <1 μM, were 5-bromo-1-ethyl-3-[(2,4-dichlorophenyl)(1 H -imidazol-1-yl)methyl]-1 H -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. [ABSTRACT FROM AUTHOR]
- Published
- 2002
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