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Probing the Role of the Covalent Linkage of Ferrocene into a Chloroquine Template

Biot, Christophe ; Daher, Wassim ; Ndiaye, Cheikh M ; Melnyk, Patricia ; Pradines, Bruno ; Chavain, Natascha ; Pellet, Alain ; Fraisse, Laurent ; Pelinski, Lydie ; Jarry, Christian ; Brocard, Jacques ; Khalife, Jamal ; Forfar-Bares, Isabelle ; Dive, Daniel

Journal of medicinal chemistry, 2006-07, Vol.49 (15), p.4707-4714 [Periódico revisado por pares]

Washington, DC: American Chemical Society

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Título:
Probing the Role of the Covalent Linkage of Ferrocene into a Chloroquine Template
Autor: Biot, Christophe ; Daher, Wassim ; Ndiaye, Cheikh M ; Melnyk, Patricia ; Pradines, Bruno ; Chavain, Natascha ; Pellet, Alain ; Fraisse, Laurent ; Pelinski, Lydie ; Jarry, Christian ; Brocard, Jacques ; Khalife, Jamal ; Forfar-Bares, Isabelle ; Dive, Daniel
Assuntos: Aminoquinolines ; Animals ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antimalarials - chemical synthesis ; Antimalarials - chemistry ; Antimalarials - pharmacology ; Antiparasitic agents ; Biological and medical sciences ; Chemical Sciences ; Chloroquine - chemistry ; Ferrous Compounds - chemical synthesis ; Ferrous Compounds - chemistry ; Ferrous Compounds - pharmacology ; Hemeproteins - antagonists & inhibitors ; Hemeproteins - chemical synthesis ; Life Sciences ; Medical sciences ; Medicinal Chemistry ; Microbiology and Parasitology ; Parasitic Sensitivity Tests ; Pharmacology. Drug treatments ; Plasmodium falciparum - drug effects ; Quinolines - chemical synthesis ; Quinolines - chemistry ; Quinolines - pharmacology ; Structure-Activity Relationship
É parte de: Journal of medicinal chemistry, 2006-07, Vol.49 (15), p.4707-4714
Notas: ark:/67375/TPS-G5XTMJSZ-B
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Descrição: 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 β-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.
Editor: Washington, DC: American Chemical Society
Idioma: Inglês

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Probing the Role of the Covalent Linkage of Ferrocene into a Chloroquine Template

Biot, Christophe ; Daher, Wassim ; Ndiaye, Cheikh M ; Melnyk, Patricia ; Pradines, Bruno ; Chavain, Natascha ; Pellet, Alain ; Fraisse, Laurent ; Pelinski, Lydie ; Jarry, Christian ; Brocard, Jacques ; Khalife, Jamal ; Forfar-Bares, Isabelle ; Dive, Daniel

Washington, DC: American Chemical Society

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