Citation: Jia-Kuo Liu, Wei Gu, Xiao-Rui Cheng, Jun-Ping Cheng, Wen-Xia Zhou, Ai-Hua Nie. Design and synthesis of cyclic acylguanidines as BACE1 inhibitors[J]. Chinese Chemical Letters, ;2015, 26(10): 1327-1330. doi: 10.1016/j.cclet.2015.07.020 shu

Design and synthesis of cyclic acylguanidines as BACE1 inhibitors

1.
Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China

Corresponding author: Wen-Xia Zhou, Ai-Hua Nie,
Received Date: 27 March 2015
Available Online: 22 May 2015
Fund Project: This work was supported by grants from The National Natural Science Foundation of China (No. 81172924) (No. 81172924)Beijing Municipal Natural Science Foundation (No. 7112106). (No. 7112106)

Based on the lead compound 1 reported in literature, a series of novel BACE1 inhibitors were designed and synthesized, among which compound 11 exhibited a 14-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.
- Alzheimer's disease,
- BACE1 inhibitor,
- Cyclic acylguanidine
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沈阳化工大学材料科学与工程学院沈阳 110142