KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine

被引：70

作者：

Kimura, T

Shuto, D

Kasai, S

Liu, P

Hidaka, K

Hamada, T

Hayashi, Y

Hattori, C

Asai, M

Kitazume, S

Saido, TC

Ishiura, S

Kiso, Y ^{[1
]}

机构：

[1] Kyoto Pharmaceut Univ, Ctr Frontier Res Med Sci, Dept Med Chem, Yamashina Ku, Kyoto 6078412, Japan

[2] Univ Tokyo, Grad Sch Arts & Sci, Dept Life Sci, Meguro Ku, Tokyo 1538902, Japan

[3] RIKEN, Frontier Res Syst, Suprabiomol Syst Grp, Glycochain Funct Lab, Wako, Saitama 3510198, Japan

[4] RIKEN, Brain Sci Inst, Lab Proteolyt Neurosci, Wako, Saitama 35101, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 06期

关键词：

D O I：

10.1016/j.bmcl.2003.12.088

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Recently, we reported a novel substrate-based octapeptide BACE1 inhibitor KMI-008 containing hydroxy-methylcarbonyl (HMC) isostere as a transition-state mimic. Using KMI-008 as a lead compound, a small-sized and highly potent BACE I inhibitor KMI-370 (IC50 = 3.4 nM) was designed and synthesized. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：1527 / 1531

页数：5

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