Synthesis and antileishmanial activity of 3-(α-azolylbenzyl)indoles

Pascal Marchand, Marc Le Borgne*, Young Min Na, Fabrice Pagniez, Hiam Abdala, Guillaume Le Baut, Patrice Le Pape

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

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 IC50<1 μM, were 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.

Original languageEnglish (US)
Pages (from-to)353-358
Number of pages6
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume17
Issue number6
DOIs
StatePublished - Dec 2002

Keywords

  • Amastigotes
  • Antileishmanial agents
  • Azoles
  • Indoles
  • Promastigotes

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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