Design and synthesis of 3＇-（prop-2-yn-1-yloxy）-biphenyl substituted cyclic acylguanidine compounds as BACE1 inhibitors

Based on the lead compounds 1 and 2, a series of novel BACE1 inhibitors were designed and synthesized,among which compound 9h exhibited a 60 fold improvement in potency over the lead compound 1. This represents a good lead for the discovery of more promising BACE1 inhibitors for the potential treatm...

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Veröffentlicht in:	中国化学快报：英文版 2016 (6), p.961-963
1. Verfasser:	Jia-Kuo Liu Wei Gu Xiao-Rui Cheng Jun-Ping Cheng Ai-Hua Nie Wen-Xia Zhou
Format:	Artikel
Sprache:	eng
Schlagworte:	先导化合物合成设计抑制剂环状联苯胍酰基铅化合物
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creator	Jia-Kuo Liu Wei Gu Xiao-Rui Cheng Jun-Ping Cheng Ai-Hua Nie Wen-Xia Zhou
description	Based on the lead compounds 1 and 2, a series of novel BACE1 inhibitors were designed and synthesized,among which compound 9h exhibited a 60 fold improvement in potency over the lead compound 1. This represents a good lead for the discovery of more promising BACE1 inhibitors for the potential treatment of AD. The result also showed that the prop-2-yn-1-yloxy is a suitable fragment for modification of cyclic acylguanidine BACE1 inhibitors.
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source	ScienceDirect Journals (5 years ago - present); Alma/SFX Local Collection
subjects	先导化合物合成设计抑制剂环状联苯胍酰基铅化合物
title	Design and synthesis of 3＇-（prop-2-yn-1-yloxy）-biphenyl substituted cyclic acylguanidine compounds as BACE1 inhibitors
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