Ferroquine-derived polyamines that target resistant Plasmodium falciparum

Stringer, Tameryn ORCID: https://orcid.org/0000-0002-4439-131X, Wiesner, Lubbe and Smith, Gregory S. (2019) Ferroquine-derived polyamines that target resistant Plasmodium falciparum. European Journal of Medicinal Chemistry, 179. pp. 78-83. ISSN 0223-5234

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Abstract

Rising resistance to conventional therapies for malaria has led to the search for novel drugs and strategies with distinct mechanisms of action that may overcome this. Ferroquine is currently the gold standard as far as antimalarial metal-based drugs are concerned and is currently in phase IIb clinical trials as part of the MMV pipeline (in partnership with Sanofi) of antimalarials. It is assumed to inhibit haemozoin formation like chloroquine and maintain its activity in the resistant strain. Here we report two ferroquine-derived polyamines that target a resistant strain of Plasmodium falciparum. Furthermore, upon treatment of Plasmodium falciparum with a ferroquine-derived polyamine, cellular haem fractionation experiments reveal that the inhibition of haemozoin formation is likely not the mechanism responsible for their activity, an important result to aid further clinical development.

Item Type: Article
Uncontrolled Keywords: sdg 3 - good health and well-being ,/dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being
Faculty \ School: Faculty of Science > School of Chemistry
Related URLs:
Depositing User: LivePure Connector
Date Deposited: 19 Jul 2022 13:30
Last Modified: 12 Aug 2022 05:31
URI: https://ueaeprints.uea.ac.uk/id/eprint/86602
DOI: 10.1016/j.ejmech.2019.06.023

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