Published In

Antimicrobial Agents and Chemotherapy

Document Type

Article

Publication Date

5-2017

Subjects

Drug design, Chloroquine -- Antimalarials, Plasmodium falciparum, Malaria

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.

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.

DOI

10.1128/AAC.01913-16

Persistent Identifier

http://archives.pdx.edu/ds/psu/20923

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