Sponsor
National Institutes of Health [AI067837, AI072923, AI094959, AI114806].
Published In
Antimicrobial Agents and Chemotherapy
Document Type
Article
Publication Date
5-2017
Subjects
Drug design, Chloroquine, Antimalarials, Plasmodium falciparum, Malaria -- Treatment
Abstract
Building on our earlier work of attaching a chemosensitizer (reversal agent) to a known drug pharmacophore, we have now expanded the structure-activity relationship study to include simplified versions of the chemosensitizer. The change from two aromatic rings in this head group to a single ring does not appear to detrimentally affect the antimalarial activity of the compounds. Data from in vitro heme binding and beta-hematin inhibition assays suggest that the single aromatic RCQ compounds retain activities against Plasmodium falciparum similar to those of CQ, although other mechanisms of action may be relevant to their activities.
DOI
10.1128/AAC.01913-16
Persistent Identifier
http://archives.pdx.edu/ds/psu/20923
Citation Details
Gunsaru B, Burgess SJ, Morrill W, Kelly JX, Shomloo S, Smilkstein MJ, Liebman K, Peyton DH. 2017. Simplified reversed chloroquines to overcome malaria resistance to quinoline-based drugs. Antimicrob Agents Chemother 61:e01913-16.
Description
Copyright © 2017 Gunsaru et al. This is an open-access article distributed under the terms of the Creative Commons Attribution 4.0 International license.