[Antileishmanial activity of five 2- or 3- quinolines by enyne group]

Dakar Med. 2005;50(3):172-5.
[Article in French]

Abstract

Introduction: Leishmaniasis is an emergent orphan disease because of its co-infection with HIV AIDS. We report herein the in vitro biological evalution of five news quinolines, 2- or 3-substituted by an enyne group against Leishmania donovani (MHOM/ET/L82/LV9).

Patients and methods: The quinolines has been synthesized by using a cross-coupling reaction between a chloroenyne and an organometallic coumpound in a presence of iron a "green" catalyst. Biological evalution is realized by a colorimetric method with the use of 3-(4,5-diméthylthiazol-2,5-diphényl)-tetrazolium bromide.

Results: Determination of the inhibitory concentrations as well as the minimal inhibitory concentrations has shown that the substitution by an enyne group made it possible to have a more important antileishmanial activity. In addition, we have seen that the -2 or the -3 position of the e nyne group h ad no influence in the antileishmanial activity.

Conclusion: Thus, we have shown the real interest of these quinolines which could be favourably compared with pentamidine, which is currently the reference p roduct, and to consider the use of these quinolines in the treament of the leishmaniasis.

Publication types

  • English Abstract

MeSH terms

  • Animals
  • Antiprotozoal Agents / pharmacology*
  • Leishmania donovani / drug effects*
  • Parasitic Sensitivity Tests
  • Quinolines / pharmacology*

Substances

  • Antiprotozoal Agents
  • Quinolines