[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-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.


CONCLUSIONS
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.
Seck
M
M
Laboratoire de Chimie Organique et Thérapeutique, Faculté de Médecine de Pharmacie et d'Odonto-stomatologie, Université Cheikh Anta Diop, Dakar, Sénégal. 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
D006801:Humans; D007896:Leishmaniasis / Q000188:drug therapy*; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D011804:Quinolines