Novel endoperoxide antimalarials: synthesis, heme binding, and antimalarial activity

…, ERT Tiekink, IG Macreadie, PI Macreadie…

文献索引：Taylor, Dennis K.; Avery, Thomas D.; Greatrex, Ben W.; Tiekink, Edward R. T.; Macreadie, Ian G.; Macreadie, Peter I.; Humphries, Adam D.; Kalkanidis, Martha; Fox, Emma N.; Klonis, Nectarios; Tilley, Leann Journal of Medicinal Chemistry, 2004 , vol. 47, # 7 p. 1833 - 1839

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被引用次数: 40

摘要

We report the synthesis of a series of novel epoxy endoperoxide compounds that can be prepared in high yields in one to three steps from simple starting materials. Some of these compounds inhibit the growth of Plasmodium falciparum in vitro. Structure-activity studies indicate that an endoperoxide ring bisubstituted with saturated cyclic moieties is the pharmacophore. To study the molecular basis of the action of these novel antimalarial ...