Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II

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• 作者：Koushi Hidaka ; Tooru Kimura ; Yumi Tsuchiya ; Mami Kamiya ; Adam J. Ruben ; Ernesto Freire ; Yoshio Hayashi ; Yoshiaki Kiso
• 关键词：Malaria ; Aspartic protease ; Plasmepsin inhibitor ; Allophenylnorstatine ; Peptidomimetic
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 June 2007
• 卷：17
• 期：11
• 页码：3048-3052
• 文件大小：341 K

摘要

Based on a highly potent allophenylnorstatine-containing inhibitor, KNI-10006, against the plasmepsins of Plasmodium falciparum, we synthesized a series of tripeptide-type compounds with various N-terminal moieties and evaluated their inhibitory activities against plasmepsin II. Certain phenylacetyl derivatives exhibited extremely high affinity with K_i values of less than 0.1 nM suggesting successful hydrophobic interactions.