Projects per year
Abstract
In the pursuit of new antimalarial leads, a phenotypic screening of various commercially sourced compound libraries was undertaken by the World Health Organisation Programme for Research and Training in Tropical Diseases (WHO-TDR). We report here the detailed characterization of one of the hits from this process, TDR32750 (8a), which showed potent activity against Plasmodium falciparum K1 (EC50 similar to 9 nM), good selectivity (>2000-fold) compared to a mammalian cell line (L6), and significant activity against a rodent model of malaria when administered intraperitoneally. Structure-activity relationship studies have indicated ways in which the molecule could be optimized. This compound represents an exciting start point for a drug discovery program for the development of a novel antimalarial.
Original language | English |
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Pages (from-to) | 2975-2990 |
Number of pages | 16 |
Journal | Journal of Medicinal Chemistry |
Volume | 56 |
Issue number | 7 |
DOIs | |
Publication status | Published - 2013 |
Keywords
- DRUG
- CONDENSED RING-SYSTEMS
- DERIVATIVES
- REACTIVITY
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Dive into the research topics of 'Discovery and structure-activity relationships of pyrrolone antimalarials'. 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