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Abstract
There is an urgent need for the development of new antimalarial compounds. As a result of a phenotypic screen, several compounds with potent activity against the parasite Plasmodium falciparum were identified. Characterization of these compounds is discussed, along with approaches to optimise the physicochemical properties. The in vitro antimalarial activity of these compounds against P. falciparum K1 had EC50 values in the range of 0.09e29 mM, and generally good selectivity (typically >100-fold) compared to a mammalian cell line (L6). One example showed no significant activity against a rodent model of malaria, and more work is needed to optimise these compounds.
Original language | English |
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Pages (from-to) | 530-538 |
Number of pages | 9 |
Journal | European Journal of Medicinal Chemistry |
Volume | 103 |
DOIs | |
Publication status | Published - 20 Oct 2015 |
Keywords
- Malaria
- Medicinal chemistry
- Phenotypic hit
- Plasmodium falciparum
ASJC Scopus subject areas
- Drug Discovery
- Organic Chemistry
- Pharmacology
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Dive into the research topics of 'Discovery and optimisation studies of antimalarial phenotypic hits'. Together they form a unique fingerprint.Projects
- 1 Finished
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Aref#d: 19815. Wellcome Trust Centre for Drug Discovery (Strategic Award)
Fairlamb, A. (Investigator), Ferguson, M. (Investigator) & Frearson, J. (Investigator)
1/01/08 → 31/12/12
Project: Research