Peer-reviewed veterinary case report
Chloroquine-astemizole hybrids with potent in vitro and in vivo antiplasmodial activity.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2009
- Authors:
- Musonda, Chitalu C et al.
- Affiliation:
- Department of Chemistry
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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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/19054674/