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Bioorganic & medicinal chemistry letters

Chloroquine-astemizole hybrids with potent in vitro and in vivo antiplasmodial activity.


PMID 19054674

Abstract

A dual activity, conjugated approach has been taken to form hybrid molecules of two known antimalarial drugs, chloroquine (CQ) and the non-sedating H1 antagonist astemizole. A variety of linkers were investigated to conjugate the two agents into one molecule. Compounds 5-8 possessed improved in vitro activity against a CQ-resistant strain of Plasmodium falciparum, and examples 7 and 8 were active in vivo in mouse models of malaria.

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A2861
Astemizole, ≥98% (HPLC)
C28H31FN4O