Amino-caprolactam γ-secretase inhibitors showing potential for the treatment of Alzheimer's disease

被引：7

作者：

Neitzel, Martin L. ^{[1
]}

Aubele, Danielle L. ^{[1
]}

Marugg, Jennifer L. ^{[1
]}

Jagodzinski, Jacek J. ^{[1
]}

Konradi, Andrei W. ^{[1
]}

Pleiss, Michael A. ^{[1
]}

Szoke, Balazs ^{[2
]}

Zmolek, Wes ^{[2
]}

Goldbach, Erich ^{[2
]}

Quinn, Kevin P. ^{[2
]}

Sauer, John-Michael ^{[2
]}

Brigham, Elizabeth F. ^{[4
]}

Wallace, William ^{[3
]}

Bova, Michael P. ^{[3
]}

Hemphill, Susanna ^{[3
]}

Basi, Guriqbal ^{[3
]}

机构：

[1] Elan Pharmaceut, Dept Med Chem, San Francisco, CA 94080 USA

[2] Elan Pharmaceut, Dept Lead Finding Drug Disposit & Safety Elvaluat, San Francisco, CA 94080 USA

[3] Elan Pharmaceut, Dept Biol, San Francisco, CA 94080 USA

[4] Elan Pharmaceut, Dept Vivo Pharmacol, San Francisco, CA 94080 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 12期

关键词：

gamma-Secretase inhibitor; Alzheimer's disease; beta-Amyloid; Notch; Amino-caprolactam; DESIGN;

D O I：

10.1016/j.bmcl.2011.04.079

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Herein we describe the structure-activity relationship (SAR) of amino-caprolactam analogs derived from amino-caprolactam benzene sulfonamide 1, highlighting affects on the potency of gamma-secretase inhibition, selectivity for the inhibition of APP versus Notch processing by gamma-secretase and selected pharmakokinetic properties. Amino-caprolactams that are efficacious in reducing the cortical A beta(x-40) levels in FVB mice via a single 100 mpk IP dose are highlighted. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：3715 / 3720

页数：6

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