Design and synthesis of cyclic acylguanidines as BACE1 inhibitors

被引：0

作者：

Jia-Kuo Liu ^{[1
]}

Wei Gu ^{[1
]}

Xiao-Rui Cheng ^{[1
]}

Jun-Ping Cheng ^{[1
]}

Wen-Xia Zhou ^{[1
]}

Ai-Hua Nie ^{[1
]}

机构：

[1] Beijing Institute of Pharmacology and Toxicology

来源：

Chinese Chemical Letters | 2015年 / 26卷 / 10期

基金：

中国国家自然科学基金;

关键词：

Alzheimer’s disease; BACE1; inhibitor; Cyclic acylguanidine;

D O I：

暂无

中图分类号：

TQ460.1 [基础理论];

学科分类号：

1007 ;

摘要：

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.

引用

页码：1327 / 1330

页数：4

共 50 条

[1] Design and synthesis of cyclic acylguanidines as BACE1 inhibitors
Liu, Jia-Kuo
Gu, Wei
Cheng, Xiao-Rui
Cheng, Jun-Ping
Zhou, Wen-Xia
Nie, Ai-Hua
CHINESE CHEMICAL LETTERS, 2015, 26 (10) : 1327 - 1330
[2] Design and synthesis of 5-cyclopropyl substituted cyclic acylguanidine compounds as BACE1 inhibitors
Liu, Jia-Kuo
Gu, Wei
Cheng, Xiao-Rui
Cheng, Jun-Ping
Nie, Ai-Hua
Zhou, Wen-Xia
CHINESE CHEMICAL LETTERS, 2016, 27 (10) : 1626 - 1629
[3] Design and synthesis of 5-cyclopropyl substituted cyclic acylguanidine compounds as BACE1 inhibitors
Jia-Kuo Liu
Wei Gu
Xiao-Rui Cheng
Jun-Ping Cheng
Ai-Hua Nie
Wen-Xia Zhou
Chinese Chemical Letters, 2016, 27 (10) : 1626 - 1629
[4] Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors
Xu, Ying-zi
Yuan, Shendong
Bowers, Simeon
Hom, Roy K.
Chan, Wayman
Sham, Hing L.
Zhu, Yong L.
Beroza, Paul
Pan, Hu
Brecht, Eric
Yao, Nanhua
Lougheed, Julie
Yan, Jiangli
Tam, Danny
Ren, Zhao
Ruslim, Lany
Bova, Michael P.
Artis, Dean R.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (10) : 3075 - 3080
[5] Design and synthesis of 3'-(prop-2-yn-1-yloxy)-biphenyl substituted cyclic acylguanidine compounds as BACE1 inhibitors
Jia-Kuo Liu
Wei Gu
Xiao-Rui Cheng
Jun-Ping Cheng
Ai-Hua Nie
Wen-Xia Zhou
Chinese Chemical Letters, 2016, (06) : 961 - 963
[6] Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors
Liu, Jian
Chen, Wuyan
Xu, Yechun
Ren, Sumei
Zhang, Wei
Li, Yingxia
BIOORGANIC & MEDICINAL CHEMISTRY, 2015, 23 (09) : 1963 - 1974
[7] Design and synthesis of 3′-(prop-2-yn-l-yloxy)-biphenyl substituted cyclic acylguanidine compounds as BACE1 inhibitors
Liu, Jia-Kuo
Gu, Wei
Cheng, Xiao-Rui
Cheng, Jun-Ping
Nie, Ai-Hua
Zhou, Wen-Xia
CHINESE CHEMICAL LETTERS, 2016, 27 (06) : 961 - 963
[8] Piperazine sulfonamide BACE1 inhibitors: Design, synthesis, and in vivo characterization
Cumming, Jared
Babu, Suresh
Huang, Ying
Carrol, Carolyn
Chen, Xia
Favreau, Leonard
Greenlee, William
Guo, Tao
Kennedy, Matthew
Kuvelkar, Reshma
Le, Thuy
Li, Guoqing
McHugh, Nansie
Orth, Peter
Ozgur, Lynne
Parker, Eric
Saionz, Kurt
Stamford, Andrew
Strickland, Corey
Tadesse, Dawit
Voigt, Johannes
Zhang, Lili
Zhang, Qi
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (09) : 2837 - 2842
[9] Design and synthesis of bicyclic acetals as Beta Secretase (BACE1) inhibitors
Innocenti, Riccardo
Lenci, Elena
Menchi, Gloria
Pupi, Alberto
Trabocchi, Andrea
BIOORGANIC & MEDICINAL CHEMISTRY, 2017, 25 (19) : 5077 - 5083
[10] Synthesis and Activity of BACE1 Inhibitors with New Core Structure
Men Xiu-Feng
He Jun-Lin
Xu Liang
Cheng Jun-Ping
Zhou Jin-Wu
Cheng Xiao-Rui
Zhou Wen-Xia
Zhang Yong-Xiang
Liu Ke-Liang
CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE, 2011, 32 (02): : 316 - 321

← 1 2 3 4 5 →