Synthesis and Biological Evaluation of 5,6-Dihydro-benzo[c] acridin-7-ol Derivatives as Anti-Alzheimer's Disease Drugs

被引：5
|
作者：
Zhou, Jinpei [2 ]
Hu, Xiaowen [1 ]
Zhang, Huibin [3 ]
Qian, Hai [3 ]
Huang, Wenlong [3 ]
Qi, Fan [2 ]
Zhang, Yanchun [2 ]
机构：
[1] Nanjing Med Univ, Dept Math & Comp, Nanjing 210029, Peoples R China
[2] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China
[3] China Pharmaceut Univ, Ctr Drug Discovery, Nanjing 210009, Peoples R China
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2009年 / 6卷 / 08期
关键词：
Alzheimer's disease; Cholinesterase inhibitors; Neuroprotection; INHIBITORS;
D O I：
10.2174/157018009789353527
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The multifactorial pathogenesis of Alzheimer's disease (AD) suggests that drug treatments with two or more mechanisms of action, acting in a complementary manner, could be more efficacious to patients suffering from the disease. In an effort to develop new therapies to treat AD, a series of 5,6-dihydro-benzo[c] acridin-7-ol derivatives (5a-5q) were synthesized and evaluated for their AchE-inhibition and neuron-protection effects. Preliminary biological tests suggested that these compounds exhibited mild AchE-inhibition and commendable neuroprotection activities. Compounds 5m, 5n, 5p had noticeable neuron-protection as compared with tacrine and nimodipine.
引用
收藏
页码：623 / 628
页数：6
相关论文
共 50 条
  • [1] SYNTHESIS, STRUCTURE AND SPECTRAL PROPERTIES OF PYRYLIUM-SALTS AND THEIR DERIVATIVES .1. 5,6-DIHYDRO-BENZO(C)XANTHYLIUM SALTS
    DELIGEORGIEV, TG
    NIKOLOV, P
    TYUTYULKOV, N
    ZEITSCHRIFT FUR NATURFORSCHUNG SECTION A-A JOURNAL OF PHYSICAL SCIENCES, 1987, 42 (01): : 43 - 48
  • [2] Synthesis and biological evaluation of 2-arylbenzofuran derivatives as potential anti-Alzheimer's disease agents
    Yun, Yinling
    Miao, Yuhang
    Sun, Xiaoya
    Sun, Jie
    Wang, Xiaojing
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021, 36 (01) : 1346 - 1356
  • [3] Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer's disease agents
    Yang, Jie
    Yun, Yinling
    Miao, Yuhang
    Sun, Jie
    Wang, Xiaojing
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2020, 35 (01) : 805 - 814
  • [4] Design, synthesis and anti-Alzheimer's disease activity evaluation of C-3 arylated huperzine A derivatives
    Zhu, Xiao-Xing
    Gao, Feng
    Wan, Lin-Xi
    FITOTERAPIA, 2024, 177
  • [5] Design, Synthesis and Biological Evaluation of Scutellarein Derivatives as Potential Anti-Alzheimer's Disease Candidates Based on Metabolic Mechanism
    Song, Shu-Lin
    Li, Nian-Guang
    Tang, Yu-Ping
    Wang, Zhen-Jiang
    Qian, Li-Hua
    Tang, Hao
    Duan, Jin-Ao
    LETTERS IN DRUG DESIGN & DISCOVERY, 2012, 9 (01) : 78 - 83
  • [6] Design, synthesis and evaluation of diosgenin carbamate derivatives as multitarget anti-Alzheimer's disease agents
    Yang, Gui-Xiang
    Huang, Yan
    Zheng, Lu-Lu
    Zhang, Li
    Su, Lin
    Wu, Yu-Hang
    Li, Jie
    Zhou, Li-Cheng
    Huang, Jin
    Tang, Yun
    Wang, Rui
    Ma, Lei
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2020, 187
  • [7] Synthesis and biological evaluation of 3-arylcoumarins as potential anti-Alzheimer's disease agents
    Yang, Jie
    Zhang, Pingping
    Hu, Yuheng
    Liu, Teng
    Sun, Jie
    Wang, Xiaojing
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2019, 34 (01) : 651 - 656
  • [8] Synthesis and biological evaluation of 4-arylcoumarins as potential anti-Alzheimer's disease agents
    Yun, Yinling
    Yang, Jie
    Miao, Yuhang
    Wang, Xiaojing
    Sun, Jie
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2020, 30 (04)
  • [9] New indole derivatives as multitarget anti-Alzheimer's agents: synthesis, biological evaluation and molecular dynamics
    Azmy, Eman M.
    Nassar, Ibrahim F.
    Hagras, Mohamed
    Fawzy, Iten M.
    Hegazy, Maghawry
    Mokhtar, Mahmoud Mohamed
    Yehia, Amr Mohamed
    Ismail, Nasser S. M.
    Lashin, Walaa H.
    FUTURE MEDICINAL CHEMISTRY, 2023, 15 (06) : 473 - 495
  • [10] Synthesis and biological evaluation of 3-(4-aminophenyl)-coumarin derivatives as potential anti-Alzheimer's disease agents
    Hu, Yu-Heng
    Yang, Jie
    Zhang, Yun
    Liu, Ke-Chun
    Liu, Teng
    Sun, Jie
    Wang, Xiao-Jing
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2019, 34 (01) : 1083 - 1092
12345