Document Detail

Selection of the most promising 2-substituted quinoline as antileishmanial candidate for clinical trials.
MedLine Citation:
PMID:  18849137     Owner:  NLM     Status:  MEDLINE    
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 1000 mg/kg after a treatment by oral route at a single dose and no sign was detected at 100 mg/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.
Nashira Campos Vieira; Christine Herrenknecht; Joel Vacus; Alain Fournet; Christian Bories; Bruno Figadère; Laila Salmen Espindola; Philippe M Loiseau
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Publication Detail:
Type:  Journal Article     Date:  2008-09-25
Journal Detail:
Title:  Biomedicine & pharmacotherapy = Biomédecine & pharmacothérapie     Volume:  62     ISSN:  1950-6007     ISO Abbreviation:  Biomed. Pharmacother.     Publication Date:  2008 Dec 
Date Detail:
Created Date:  2008-11-18     Completed Date:  2009-01-19     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8213295     Medline TA:  Biomed Pharmacother     Country:  France    
Other Details:
Languages:  eng     Pagination:  684-9     Citation Subset:  IM    
Laboratoire de Pharmacognosie Groupe de et Chimiothérapie Antiparasitaire UMR 8076 CNRS, Faculté de Pharmacie, Université Paris-Sud, Rue Jean-Baptiste Clément, 92296 Châtenay-Malabry Cedex, France.
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MeSH Terms
Acute Toxicity Tests
Drug Resistance
Drug Stability
Leishmania donovani / drug effects
Parasitic Sensitivity Tests
Quinolines / administration & dosage,  chemistry*,  pharmacology
Structure-Activity Relationship
Trypanocidal Agents / administration & dosage,  chemistry*,  pharmacology
Reg. No./Substance:
0/2-propylquinoline; 0/Quinolines; 0/Trypanocidal Agents

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