Synthesis and evaluation of tacrine-E2020 hybrids as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease

被引：66
|
作者：
Shao, D [1 ]
Zou, CY [1 ]
Luo, C [1 ]
Tang, XC [1 ]
Li, YC [1 ]
机构：
[1] Chinese Acad Sci, Grad Sch, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 18期
关键词：
tacrine-E2020; hybrids; acetylcholinesterase inhibitor; Alzheimer's disease;
D O I：
10.1016/j.bmcl.2004.07.005
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Tacrine-E2020 hybrids and some related compounds were prepared and their bioactivities on the Alzheimer's disease were assayed. The optimum hybrid inhibitor 3 is 37-fold more potent and 31-fold more selective than tacrine in vitro. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4639 / 4642
页数：4
相关论文
共 50 条
  • [21] Design, synthesis and biological evaluation of dual acetylcholinesterase and phosphodiesterase 5A inhibitors in treatment for Alzheimer's disease
    Zhou, Li-yun
    Zhu, Yao
    Jiang, Yu-ren
    Zhao, Xiong-jie
    Guo, Dong
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (17) : 4180 - 4184
  • [22] Design, synthesis, and biological evaluation of novel capsaicin-tacrine hybrids as multi-target agents for the treatment of Alzheimer's disease
    Long, Juanyue
    Qin, Fengxue
    Luo, Jinchong
    Zhong, Guohui
    Huang, Shutong
    Jing, Lin
    Yi, Tingzhuang
    Liu, Jing
    Jiang, Neng
    BIOORGANIC CHEMISTRY, 2024, 143
  • [23] Molecular evaluation of herbal compounds as potent inhibitors of acetylcholinesterase for the treatment of Alzheimer's disease
    Chen, Yan-Xiu
    Li, Guan-Zeng
    Zhang, Bin
    Xia, Zhang-Yong
    Zhang, Mei
    MOLECULAR MEDICINE REPORTS, 2016, 14 (01) : 446 - 452
  • [24] Design and synthesis of novel flavonoid derivatives as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease
    Kranzlein, Anna
    Newman, Olivia
    Mills, Chavonda J.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2014, 247
  • [25] Design and synthesis of tacrine-phenothiazine hybrids as multitarget drugs for Alzheimer’s disease
    Ai-ling Hui
    Yan Chen
    Shi-jing Zhu
    Chang-sheng Gan
    Jian Pan
    An Zhou
    Medicinal Chemistry Research, 2014, 23 : 3546 - 3557
  • [26] Design and synthesis of tacrine-phenothiazine hybrids as multitarget drugs for Alzheimer's disease
    Hui, Ai-ling
    Chen, Yan
    Zhu, Shi-jing
    Gan, Chang-sheng
    Pan, Jian
    Zhou, An
    MEDICINAL CHEMISTRY RESEARCH, 2014, 23 (07) : 3546 - 3557
  • [27] Synthesis and characterization of novel flavonoid derivatives as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease
    DePhillips, Jessica
    Martin, Sarah
    Denning, Andrew
    Minnick, Jennifer
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2017, 253
  • [28] Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease
    Marco-Contelles, Jose
    Leon, Rafael
    de los Rios, Cristobal
    Guglietta, Antonio
    Terencio, Jose
    Lopez, Manuela G.
    Garcia, Antonio G.
    Villarroya, Mercedes
    JOURNAL OF MEDICINAL CHEMISTRY, 2006, 49 (26) : 7607 - 7610
  • [29] Acetylcholinesterase inhibitors in Alzheimer's disease
    McGleenon, BM
    Dynan, KB
    Passmore, AP
    BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1999, 48 (04) : 471 - 480
  • [30] The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer's Disease
    Vecchio, Immacolata
    Sorrentino, Luca
    Paoletti, Annamaria
    Marra, Rosario
    Arbitrio, Mariamena
    JOURNAL OF CENTRAL NERVOUS SYSTEM DISEASE, 2021, 13
12345