| Selection of the most promising 2-substituted quinoline as antileishmanial candidate for clinical trials. | |
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MedLine Citation:
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PMID: 18849137 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: Journal Article Date: 2008-09-25 |
Journal Detail:
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Title: Biomedicine & pharmacotherapy = Biomédecine & pharmacothérapie Volume: 62 ISSN: 1950-6007 ISO Abbreviation: Biomed. Pharmacother. Publication Date: 2008 Dec |
Date Detail:
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Created Date: 2008-11-18 Completed Date: 2009-01-19 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8213295 Medline TA: Biomed Pharmacother Country: France |
Other Details:
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Languages: eng Pagination: 684-9 Citation Subset: IM |
Affiliation:
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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. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Acute Toxicity Tests Animals 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 |
| Chemical | |
Reg. No./Substance:
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0/2-propylquinoline; 0/Quinolines; 0/Trypanocidal Agents |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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