| Probing the role of the covalent linkage of ferrocene into a chloroquine template. | |
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MedLine Citation:
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PMID: 16854077 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A new therapeutic approach to malaria led to the discovery of ferroquine (FQ, SR97276). To assess the importance of the linkage of the ferrocenyl group to a 4-aminoquinoline scaffold, two series of 4-aminoquinolines, structurally related to FQ, were synthesized. Evaluation of antimalarial activity, physicochemical parameters, and the beta-hematin inhibition property indicate that the ferrocene moiety has to be covalently flanked by a 4-aminoquinoline and an alkylamine. Current data reinforced our choice of FQ as a drug candidate. |
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Authors:
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Christophe Biot; Wassim Daher; Cheikh M Ndiaye; Patricia Melnyk; Bruno Pradines; Natascha Chavain; Alain Pellet; Laurent Fraisse; Lydie Pelinski; Christian Jarry; Jacques Brocard; Jamal Khalife; Isabelle Forfar-Bares; Daniel Dive |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 49 ISSN: 0022-2623 ISO Abbreviation: J. Med. Chem. Publication Date: 2006 Jul |
Date Detail:
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Created Date: 2006-07-20 Completed Date: 2006-08-31 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: United States |
Other Details:
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Languages: eng Pagination: 4707-14 Citation Subset: IM |
Affiliation:
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Unité de Catalyse et Chimie du Solide - UMR CNRS 8181, ENSCL, Bâtiment C7, USTL, B.P. 90108, 59652, Villeneuve d' Ascq Cedex, France. christophe.biot@ensc-lille.fr |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Aminoquinolines Animals Antimalarials / chemical synthesis*, chemistry, pharmacology Chloroquine / chemistry* Ferrous Compounds / chemical synthesis*, chemistry, pharmacology Hemeproteins / antagonists & inhibitors, chemical synthesis Parasitic Sensitivity Tests Plasmodium falciparum / drug effects Quinolines / chemical synthesis*, chemistry, pharmacology Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Aminoquinolines; 0/Antimalarials; 0/Ferrous Compounds; 0/Hemeproteins; 0/Quinolines; 0/ferroquine; 39404-00-7/hemozoin; 54-05-7/Chloroquine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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