Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating d-cysteine derivatives as P₂/P₃ moieties

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• 作者：Ei’ ; ichi Ami ; Koichiro Nakahara ; Akihiko Sato ; Jeffrey-Tri Nguyen ; Koushi Hidaka ; Yoshio Hamada ; Shingo Nakatani ; Tooru Kimura ; Yoshio Hayashi ; Yoshiaki Kiso
• 关键词：HIV protease ; Protease inhibitor ; Drug-resistant HIV strain ; d-Cysteine ; Allophenylnorstatine
• 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 August 2007
• 卷：17
• 期：15
• 页码：4213-4217
• 文件大小：291 K

摘要

We designed several HIV protease inhibitors with various d-cysteine derivatives as P₂/P₃ moieties based on the structure of clinical drug candidate, KNI-764. Herein, we report their synthesis, HIV protease inhibitory activity, HIV IIIB cell inhibitory activity, cellular toxicity, and inhibitory activity against drug-resistant HIV strains. KNI-1931 showed distinct selectivity against HIV proteases and high potency against drug-resistant strains, surpassing those of Ritonavir and Nelfinavir.