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• W2107013886 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 (EC(50) ~ 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." @default.
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• W2107013886 date "2013-03-21" @default.
• W2107013886 modified "2023-09-29" @default.
• W2107013886 title "Discovery and Structure–Activity Relationships of Pyrrolone Antimalarials" @default.
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• W2107013886 doi "https://doi.org/10.1021/jm400009c" @default.
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