Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: Exploration of P1 phenoxy and benzyloxy residues
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- 作者：Marcus Bä ; ck ; Jonas Nyhlé ; n ; Ingemar Kvarnströ ; m ; Sara Appelgren ; Neera Borkakoti ; Katarina Jansson ; Jimmy Lindberg ; Susanne Nyströ ; m ; Anders Hallberg ; Å ; sa Rosenquist ; Bertil Samu
- 关键词：Alzheimer’ ; s disease ; BACE-1 inhibitors ; P1 modifications ; Peptidomimetics
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2008
- 出版时间：1 November 2008
- 年：2008
- 卷：16
- 期：21
- 页码：9471-9486
- 全文大小：419 K
文摘
Several BACE-1 inhibitors with low nanomolar level activities, encompassing a statine-based core structure with phenyloxymethyl- and benzyloxymethyl residues in the P1 position, are presented. The novel P1 modification introduced to allow the facile exploration of the S1 binding pocket of BACE-1, delivered highly promising inhibitors.