Selection of the most promising 2-substituted quinoline as antileishmanial candidate for clinical trials - 26/11/08
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Abstract |
The antileishmanial evaluation of more than one hundred 2-substituted quinolines led us to identify three compounds for further studies: compound 1 (2-n-propylquinoline), compound 2 (2-(2methoxyethenyl)quinoline) and compound 3 (2-(2-hydroxyprop-2-enyl)quinoline). The final selection of a potential drug candidate was mainly based on chemical stability and acute oral toxicity as discriminating criteria. The most stable compound in various conditions was 2-n-propylquinoline (compound 1). Only reversible toxicity signs were observed for compound 1 at 1000mg/kg after a treatment by oral route at a single dose and no sign was detected at 100mg/kg. Interestingly, 2-substituted quinolines were active on a Leishmania donovani line, resistant to sitamaquine, a 8-aminoquinoline, suggesting that 2-substituted quinolines and 8-aminoquinoline probably affect a different target in L. donovani.
Le texte complet de cet article est disponible en PDF.Keywords : 2-Substituted quinolines, Leishmaniasis, Chemical stability
Plan
Vol 62 - N° 10
P. 684-689 - décembre 2008 Retour au numéroBienvenue sur EM-consulte, la référence des professionnels de santé.
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