Seck M, Desrivot J, Bories C, Loiseau P, Franck X, Hocquemiller R, Figadere B, Peyrat J F, Provot O, Brion J D, Alami M
Laboratoire de Chimie Organique et Thérapeutique, Faculté de Médecine de Pharmacie et d'Odonto-stomatologie, Université Cheikh Anta Diop, Dakar, Sénégal.
Dakar Med. 2006;51(1):1-4.
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).
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.
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.
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.
利什曼病由于与艾滋病毒/艾滋病合并感染，已成为一种新出现的孤儿病。我们在此报告5种新喹啉的体外生物学评价，这些喹啉在2位或3位被烯炔基取代，针对杜氏利什曼原虫（MHOM/ET/L82/LV9）。
喹啉是通过在“绿色”催化剂铁的存在下，使氯烯炔与有机金属化合物之间发生交叉偶联反应合成的。生物学评价通过使用3-(4,5-二甲基噻唑-2,5-二苯基)-溴化四氮唑的比色法来实现。
抑制浓度以及最小抑制浓度的测定表明，被烯炔基取代使得具有更重要的抗利什曼活性成为可能。此外，我们发现烯炔基的-2或-3位对抗利什曼活性没有影响。
因此，我们已经表明这些喹啉具有实际价值，它们可以与目前作为参考产品的喷他脒进行有利比较，并考虑在利什曼病治疗中使用这些喹啉。
