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High antiplasmodial activity of novel plasmepsins I and II inhibitors

M Dell'Agli, S Parapini, G Galli, N Vaiana…

文献索引:Dell'Agli, Mario; Parapini, Silvia; Galli, Germana; Vaiana, Nadia; Taramelli, Donatella; Sparatore, Anna; Liu, Peng; Dunn, Ben M.; Bosisio, Enrica; Romeo, Sergio Journal of Medicinal Chemistry, 2006 , vol. 49, # 25 p. 7440 - 7449

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被引用次数: 29

摘要

The aim of this study was to develop new antiplasmodial compounds acting through distinct mechanisms during both the liver and the blood stages of the parasite life cycle. Compounds were designed on the basis of the “double-drug” approach: primaquine, which has been linked to statine-based inhibitors of plasmepsins (PLMs), the plasmodial aspartic proteases involved in degradation of hemeoglobin. The compounds were tested in vitro for anti-PLM ...