Potent pyrrolidine- and piperidine-based BACE-1 inhibitors

被引：72

作者：

Iserloh, U. ^{[1
]}

Wu, Y. ^{[1
]}

Cumming, J. N. ^{[1
]}

Pan, J. ^{[1
]}

Wang, L. Y. ^{[1
]}

Stamford, A. W. ^{[1
]}

Kennedy, M. E. ^{[2
]}

Kuvelkar, R. ^{[2
]}

Chen, X. ^{[2
]}

Parker, E. M. ^{[2
]}

Strickland, C. ^{[1
]}

Voigt, J. ^{[1
]}

机构：

[1] Schering Plough Res Inst, Dept Chem Res, Kenilworth, NJ 07033 USA

[2] Schering Plough Res Inst, Dept Neurobiol, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 01期

关键词：

D O I：

10.1016/j.bmcl.2007.10.116

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Based on lead compound I identified from the patent literature, we developed novel patentable BACE-1 inhibitors by introducing a cyclic amine scaffold. Extensive SAR studies on both pyrrolidines and piperidines ultimately led to inhibitor 2f, one of the most potent inhibitors synthesized to date. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：414 / 417

页数：4

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