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Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter

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 a...

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Detalles Bibliográficos
Autores principales: Egan, Timothy J, Kuter, David
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Future Medicine Ltd 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7099626/
https://www.ncbi.nlm.nih.gov/pubmed/23534360
http://dx.doi.org/10.2217/fmb.13.18
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author Egan, Timothy J
Kuter, David
author_facet Egan, Timothy J
Kuter, David
author_sort Egan, Timothy J
collection PubMed
description 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.
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spelling pubmed-70996262020-03-27 Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter Egan, Timothy J Kuter, David Future Microbiol Review 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. Future Medicine Ltd 2013-04 2013-03-27 /pmc/articles/PMC7099626/ /pubmed/23534360 http://dx.doi.org/10.2217/fmb.13.18 Text en © 2013 Future Medicine Ltd This work is licensed under the Creative Commons Attribution 4.0 License (http://creativecommons.org/licenses/by/4.0/)
spellingShingle Review
Egan, Timothy J
Kuter, David
Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter
title Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter
title_full Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter
title_fullStr Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter
title_full_unstemmed Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter
title_short Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter
title_sort dual-functioning antimalarials that inhibit the chloroquine-resistance transporter
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7099626/
https://www.ncbi.nlm.nih.gov/pubmed/23534360
http://dx.doi.org/10.2217/fmb.13.18
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