Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aminoquinolines
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Animals
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Antimalarials / chemical synthesis*
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Antimalarials / chemistry
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Antimalarials / pharmacology
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Chloroquine / chemistry*
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Ferrous Compounds / chemical synthesis*
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Ferrous Compounds / chemistry
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Ferrous Compounds / pharmacology
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Hemeproteins / antagonists & inhibitors
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Hemeproteins / chemical synthesis
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Metallocenes
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Parasitic Sensitivity Tests
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Plasmodium falciparum / drug effects
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Quinolines / chemical synthesis*
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Quinolines / chemistry
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Quinolines / pharmacology
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Structure-Activity Relationship
Substances
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Aminoquinolines
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Antimalarials
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Ferrous Compounds
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Hemeproteins
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Metallocenes
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Quinolines
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hemozoin
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Chloroquine
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ferroquine