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

CC Musonda, GA Whitlock, MJ Witty, R Brun…

Index: Musonda, Chitalu C.; Whitlock, Gavin A.; Witty, Michael J.; Brun, Reto; Kaiser, Marcel Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 2 p. 481 - 484

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Citation Number: 30

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 ...

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