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[Antileishmanial activity of five 2- or 3- quinolines by enyne group]. 2005

M Seck, and J Desrivot, and C Bories, and P Loiseau, and X Franck, and R Hocquemiller, and B Figadere, and J F Peyrat, and O Provot, and J D Brion, and M Alami
Laboratoire de Chimie Organique et Thérapeutique, Faculté de Medecine de Pharmacie et d'Odonto-stomatologie, Université. matarsec@yahoo.fr

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.

UI MeSH Term Description Entries
D007893 Leishmania donovani A parasitic hemoflagellate of the subgenus Leishmania leishmania that infects man and animals and causes visceral leishmaniasis (LEISHMANIASIS, VISCERAL). The sandfly genera Phlebotomus and Lutzomyia are the vectors. Leishmania (Leishmania) donovani,Leishmania leishmania donovani,Leishmania donovanus,Leishmania leishmania donovanus,donovani, Leishmania leishmania,donovanus, Leishmania,donovanus, Leishmania leishmania,leishmania donovanus, Leishmania
D011804 Quinolines
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000981 Antiprotozoal Agents Substances that are destructive to protozoans. Schizonticides,Agents, Antiprotozoal
D021261 Parasitic Sensitivity Tests Tests that demonstrate the relative effectiveness of chemotherapeutic agents against specific parasites. Drug Sensitivity Tests, Helminth,Drug Sensitivity Tests, Parasitic,Drug Sensitivity Tests, Protozoal,Helminth Drug Sensitivity Tests,Parasite Sensitivity Tests,Protozoa Drug Sensitivity Tests,Protozoal Drug Sensitivity Tests,Parasite Sensitivity Test,Parasitic Sensitivity Test,Sensitivity Test, Parasite,Sensitivity Test, Parasitic,Sensitivity Tests, Parasite,Test, Parasite Sensitivity,Test, Parasitic Sensitivity,Tests, Parasite Sensitivity,Tests, Parasitic Sensitivity

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