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


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.


CONCLUSIONS
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.
Seck
M
M
Laboratoire de Chimie Organique et Thérapeutique, Faculté de Medecine de Pharmacie et d'Odonto-stomatologie, Université. matarsec@yahoo.fr
Desrivot
J
J
Bories
C
C
Loiseau
P
P
Franck
X
X
Hocquemiller
R
R
Figadere
B
B
Peyrat
J F
JF
Provot
O
O
Brion
J D
JD
Alami
M
M
D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D007893:Leishmania donovani / Q000187:drug effects*; D021261:Parasitic Sensitivity Tests; D011804:Quinolines / Q000494:pharmacology*
D000981:Antiprotozoal Agents; D011804:Quinolines