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J Med Chem. 2007 Feb 22;50(4):595-8. Epub 2007 Jan 31.

Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore.

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Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universita' di Siena, via Aldo Moro, 53100 Siena, Italy.


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.

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