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

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
19
Issue
2
Identifiers
DOI: 10.1016/j.bmcl.2008.11.047
Keywords
  • Malaria
  • Hybrid
  • Plasmodium Falciparum
  • Conjugated Approach

Abstract

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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