Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter.

Abstract:

: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.

journal_name

Future Microbiol

journal_title

Future microbiology

authors

Egan TJ,Kuter D

doi

10.2217/fmb.13.18

subject

Has Abstract

pub_date

2013-04-01 00:00:00

pages

475-89

issue

4

eissn

1746-0913

issn

1746-0921

journal_volume

8

pub_type

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