Citation: Jia-Kuo Liu, Wei Gu, Xiao-Rui Cheng, Jun-Ping Cheng, Ai-Hua Nie, Wen-Xia Zhou. Design and synthesis of 3'-(prop-2-yn-1-yloxy)-biphenyl substituted cyclic acylguanidine compounds as BACE1 inhibitors[J]. Chinese Chemical Letters, ;2016, 27(6): 961-963. doi: 10.1016/j.cclet.2016.02.006 shu

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

Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China

Received Date: 30 November 2015
Revised Date: 23 December 2015

Fund Project: This work was supported by grants from The National Natural Science Foundation of China (No. 81172924) and Beijing Municipal Natural Science Foundation (No. 7112106).

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.
- Alzheimer's disease,
- BACE1 inhibitor,
- Prop-2-yn-1-yloxy,
- Cyclic acylguanidine
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