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. 2009 Jan 15;19(2):481-4.
doi: 10.1016/j.bmcl.2008.11.047. Epub 2008 Nov 18.

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

Chitalu C Musonda  1 , Gavin A Whitlock, Michael J Witty, Reto Brun, Marcel Kaiser
Affiliations

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

Chitalu C Musonda et al. Bioorg Med Chem Lett. .

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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