Discovery, synthesis, and optimization of antimalarial 4 (1 H)-quinolone-3-diarylethers

…, S Pou, AM Pershing, AM Stickles, E Ryan…

文献索引：Nilsen, Aaron; Miley, Galen P.; Forquer, Isaac P.; Mather, Michael W.; Katneni, Kasiram; Li, Yuexin; Pou, Sovitj; Pershing, April M.; Stickles, Allison M.; Ryan, Eileen; Kelly, Jane Xu; Doggett, J. Stone; White, Karen L.; Hinrichs, David J.; Winter, Rolf W.; Charman, Susan A.; Zakharov, Lev N.; Bathurst, Ian; Burrows, Jeremy N.; Vaidya, Akhil B.; Riscoe, Michael K. Journal of Medicinal Chemistry, 2014 , vol. 57, # 9 p. 3818 - 3834

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被引用次数: 28

摘要

The historical antimalarial compound endochin served as a structural lead for optimization. Endochin-like quinolones (ELQ) were prepared by a novel chemical route and assessed for in vitro activity against multidrug resistant strains of Plasmodium falciparum and against malaria infections in mice. Here we describe the pathway to discovery of a potent class of orally active antimalarial 4 (1 H)-quinolone-3-diarylethers. The initial prototype, ELQ-233, ...