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Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter.
MedLine Citation:
PMID:  23534360     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
Malaria remains a major international health challenge. Resistance to a number of existing drugs and evidence of the emergence of artemisinin resistance has emphasized the need for new antimalarials. A new approach has been the preparation of dual-function compounds that include a chloroquine-like antimalarial group and a group that resembles a chloroquine chemosensitizer. This article reviews the recent discovery of such dual-function antimalarials that are proposed to target both hemozoin formation and the chloroquine resistance transporter, PfCRT. These are discussed in relation to the mechanism of action of 4-aminoquinolines, chloroquine resistance and resistance reversal.
Authors:
Timothy J Egan; David Kuter
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Future microbiology     Volume:  8     ISSN:  1746-0921     ISO Abbreviation:  Future Microbiol     Publication Date:  2013 Apr 
Date Detail:
Created Date:  2013-03-28     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101278120     Medline TA:  Future Microbiol     Country:  England    
Other Details:
Languages:  eng     Pagination:  475-89     Citation Subset:  IM    
Affiliation:
Department of Chemistry, University of Cape Town, Private Bag, Rondebosch 7701, South Africa.
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