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

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.

• Authors: M Seck, J Desrivot, C Bories, P Loiseau, X Franck, R Hocquemiller, B Figadere, J F Peyrat, O Provot, J D Brion, M Alami
• Journal: Dakar medical (Dakar Med) Vol. 50 Issue 3 Pg. 172-5 ( 2005) ISSN: 0049-1101 [Print] Senegal
• Vernacular Title: Activité anti leishmanienne de cinq quinoléines substituées en position 2- ou 3- par un groupement ényne.
• PMID: 17633005 (Publication Type: English Abstract, Journal Article)

Chemical References

• Antiprotozoal Agents
• Quinolines

Topics

• Animals
• Antiprotozoal Agents (pharmacology)
• Leishmania donovani (drug effects)
• Parasitic Sensitivity Tests
• Quinolines (pharmacology)