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.
| Original language | English |
|---|---|
| Pages (from-to) | 78-83 |
| Number of pages | 6 |
| Journal | European Journal of Medicinal Chemistry |
| Volume | 179 |
| Early online date | 8 Jun 2019 |
| DOIs | |
| Publication status | Published - 1 Oct 2019 |
UN SDGs
This output contributes to the following UN Sustainable Development Goals (SDGs)
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SDG 3 Good Health and Well-being
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