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首页> 外文期刊>Journal of Medicinal Chemistry >Design and Synthesis of Plasmepsin I and Plasmepsin II Inhibitors with Activity in Plasmodium falciparum-Infected Cultured Human Erythrocytes
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Design and Synthesis of Plasmepsin I and Plasmepsin II Inhibitors with Activity in Plasmodium falciparum-Infected Cultured Human Erythrocytes

机译：在恶性疟原虫感染的培养人红细胞中具有活性的纤溶酶I和纤溶酶II抑制剂的设计与合成

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摘要

A series of protease inhibitors targeted at the malarial enzymes plasmepsin I and II, and encompassing a basic hydroxyethylamine transition state isostere scaffold, was prepared. The substituents in the P1' position were varied and the biological activities expressed in K_i-values ranged from 60 to >2000 nM. A more than 4-fold selectivity for either of the plasmepsins could be achieved. All of the active compounds exhibited high preference for the plasmepsins over cathepsin D, the most closely related human protease. A few active compounds were shown to inhibit parasite growth in cultured infected human erythrocytes. An ED_(50) value as low as 1.6 μM was observed for one of the inhibitors despite K_i values of 115 nM (Plm I) and 121 nM (Plm II).
机译：制备了一系列针对疟疾纤溶酶I和II的蛋白酶抑制剂，包括碱性羟乙胺过渡态等排骨架。在P1'位置的取代基是变化的，并且以K_i值表示的生物活性为60至> 2000nM。对于任一纤溶酶而言，可以实现超过4倍的选择性。与组织蛋白酶D（最密切相关的人类蛋白酶）相比，所有活性化合物均对纤溶酶表现出更高的偏爱。几种活性化合物显示抑制培养的感染人类红细胞中的寄生虫生长。尽管K_i值为115 nM（Plm I）和121 nM（Plm II），但其中一种抑制剂的ED_（50）值仍低至1.6μM。

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