| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375880 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
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.
Graphical abstractA series of novel hybrids of CQ and astemizole have been shown to possess potent in vitro and in vivo antiplasmodial activity.Figure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Chitalu C. Musonda, Gavin A. Whitlock, Michael J. Witty, Reto Brun, Marcel Kaiser,