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Updated: Jul 20, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
[Antileishmanial activity of five 2- or 3- quinolines by enyne group]
1Laboratoire de Chimie Organique et Thérapeutique, Faculté de Médecine de Pharmacie et d'Odonto-stomatologie, Université Cheikh Anta Diop, Dakar, Sénégal. matarsec@yahoo.fr
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-dimethylthiazol-2,5-diphényl)-tétrazolium 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 enyne group had 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 product, and to consider the use of these quinolines in the treament of the leishmaniasis.
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