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
  • [1] Synthesis and evaluation of tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease
    Badia, A
    Banos, JE
    Camps, P
    Contreras, J
    Gorbig, DM
    Munoz-Torrero, D
    Simon, M
    Vivas, NM
    BIOORGANIC & MEDICINAL CHEMISTRY, 1998, 6 (04) : 427 - 440
  • [2] Novel tacrine-based acetylcholinesterase inhibitors as potential agents for the treatment of Alzheimer’s disease: Quinolotacrine hybrids
    Mehrdad Sadafi Kohnehshahri
    Gholamabbas Chehardoli
    Masoomeh Bahiraei
    Tahmineh Akbarzadeh
    Akram Ranjbar
    Arezoo Rastegari
    Zahra Najafi
    Molecular Diversity, 2022, 26 : 489 - 503
  • [3] Novel tacrine-based acetylcholinesterase inhibitors as potential agents for the treatment of Alzheimer's disease: Quinolotacrine hybrids
    Sadafi Kohnehshahri, Mehrdad
    Chehardoli, Gholamabbas
    Bahiraei, Masoomeh
    Akbarzadeh, Tahmineh
    Ranjbar, Akram
    Rastegari, Arezoo
    Najafi, Zahra
    MOLECULAR DIVERSITY, 2022, 26 (01) : 489 - 503
  • [4] Synthesis, in vitro pharmacology, and molecular modeling of very potent tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease
    Camps, P
    El Achab, R
    Görbig, DM
    Morral, J
    Muñoz-Torrero, D
    Badia, A
    Baños, JE
    Vivas, NM
    Barril, X
    Orozco, M
    Luque, FJ
    JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (17) : 3227 - 3242
  • [5] Design Synthesis and in vitro Evaluation of Tacrine-flavone Hybrids as Multifunctional Cholinesterase Inhibitors for Alzheimer's Disease
    Remya, R. S.
    Ramalakshmi, N.
    Nalini, C. N.
    Niraimathi, V
    Amuthalakshmi, S.
    CURRENT COMPUTER-AIDED DRUG DESIGN, 2022, 18 (04) : 271 - 292
  • [6] Design, synthesis and evaluation of novel tacrine coumarin hybrids as multifunctional cholinesterase inhibitors against Alzheimer's disease
    Xie, Sai-Sai
    Wang, Xiao-Bing
    Li, Jiang-Yan
    Yang, Lei
    Kong, Ling-Yi
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 64 : 540 - 553
  • [7] Design, synthesis and evaluation of novel tacrine rhein hybrids as multifunctional agents for the treatment of Alzheimer's disease
    Li, Su-Yi
    Jiang, Neng
    Xie, Sai-Sai
    Wang, Kelvin D. G.
    Wang, Xiao-Bing
    Kong, Ling-Yi
    ORGANIC & BIOMOLECULAR CHEMISTRY, 2014, 12 (05) : 801 - 814
  • [8] New tacrine-hydrazinonicotinamide hybrids as acetylcholinesterase inhibitors of potential interest for the early diagnostics of Alzheimer's disease
    Szymanski, P
    Zurek, E
    Mikiciuk-Olasik, E
    PHARMAZIE, 2006, 61 (04): : 269 - 273
  • [9] Synthesis and biological evaluation of novel fluorinated tacrine hybrids against Alzheimer's disease
    Obi, Chibuike
    Sledge, Alexis
    Okoro, Cosmas
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2016, 252
  • [10] Design, synthesis and evaluation of novel tacrine-(β-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease
    Lan, Jin-Shuai
    Xie, Sai-Sai
    Li, Su-Yi
    Pan, Long-Fei
    Wang, Xiao-Bing
    Kong, Ling-Yi
    BIOORGANIC & MEDICINAL CHEMISTRY, 2014, 22 (21) : 6089 - 6104
12345