Abstract | INTRODUCTION: 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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Authors | M Seck, J Desrivot, C Bories, P Loiseau, X Franck, R Hocquemiller, B Figadere, J F Peyrat, O Provot, J D Brion, M Alami |
Journal | Dakar medical
(Dakar Med)
Vol. 51
Issue 1
Pg. 1-4
( 2006)
ISSN: 0049-1101 [Print] Senegal |
Vernacular Title | Activité anti leishmanienne de cinq quinoléines substitutées en position 2- ou 3- par un groupement, enyne. |
PMID | 16924841
(Publication Type: English Abstract, Journal Article)
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Chemical References |
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Topics |
- Humans
- Leishmaniasis
(drug therapy)
- Molecular Structure
- Quinolines
(chemical synthesis, pharmacology)
- Structure-Activity Relationship
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