Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: Exploration of P1 phenoxy and benzyloxy residues
Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: Exploration of P1 phenoxy and benzyloxy residues
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DOI：
10.1016/j.bmc.2008.09.041
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发表时间：
2008-11-01
影响因子：
3.5
通讯作者：
Samuelsson, Bertil
中科院分区：
文献类型：
--
作者：
Back, Marcus;Nyhlen, Jonas;Samuelsson, Bertil
几个BACE-1抑制剂与低纳摩尔水平的活动，包括他汀类药物为基础的核心结构与苯氧基甲基和苄氧基甲基残基的P1位置，提出。小说P1 Modi.引入阳离子以允许容易地探索BACE-1的S1结合口袋，提供了非常有前途的抑制剂。(C)2008爱思唯尔有限公司保留所有权利。
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 modi. cation introduced to allow the facile exploration of the S1 binding pocket of BACE-1, delivered highly promising inhibitors. (C) 2008 Elsevier Ltd. All rights reserved.