Abstract
Identification of new molecular scaffolds structurally unrelated to known antimalarials may represent a valid strategy to overcome resistance of P. falciparum (Pf) to currently available drugs. We describe herein the investigation of a new polycyclic pharmacophore, related to clotrimazole, to develop innovative antimalarial agents. This study allowed us to discover compounds characterized by a high in vitro potency, particularly against Pf CQ-resistant strains selectively targeting free heme, which are easy to synthesize by low-cost synthetic strategies.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antifungal Agents / chemical synthesis
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Antifungal Agents / pharmacology
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Antimalarials / chemical synthesis*
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Antimalarials / pharmacology
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Cell Line
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Clotrimazole / analogs & derivatives*
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Clotrimazole / chemical synthesis*
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Clotrimazole / pharmacology
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Drug Resistance
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Heterocyclic Compounds, 4 or More Rings / chemical synthesis*
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Heterocyclic Compounds, 4 or More Rings / pharmacology
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Humans
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In Vitro Techniques
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Models, Molecular
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Plasmodium falciparum / drug effects
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Structure-Activity Relationship
Substances
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Antifungal Agents
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Antimalarials
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Heterocyclic Compounds, 4 or More Rings
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Clotrimazole