Rational approach to discover multipotent anti-Alzheimer drugs

被引:232
|
作者
Rosini, M
Andrisano, V
Bartolini, M
Bolognesi, ML
Hrelia, P
Minarini, A
Tarozzi, A
Melchiorre, C
机构
[1] Univ Bologna, Dept Pharmaceut Sci, I-40126 Bologna, Italy
[2] Univ Bologna, Dept Pharmacol, I-40126 Bologna, Italy
关键词
D O I
10.1021/jm049112h
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The coupling of two different pharmacophores, each endowed with different biological properties, afforded the hybrid compound lipocrine (7), whose biological profile was markedly improved relative to those of prototypes tacrine and lipoic acid. Lipocrine is the first compound that inhibits the catalytic activity of AChE and AChE-induced amyloid-beta aggregation and protects against reactive oxygen species. Thus, it emerged as a valuable pharmacological tool to investigate Alzheimer's disease and as a promising lead compound for new anti-Alzheimer drugs.
引用
收藏
页码:360 / 363
页数:4
相关论文
共 50 条
  • [21] Novel Tacrine-Grafted Ugi Adducts as Multipotent Anti-Alzheimer Drugs: A Synthetic Renewal in Tacrine-Ferulic Acid Hybrids
    Benchekroun, Mohamed
    Bartolini, Manuela
    Egea, Javier
    Romero, Alejandro
    Soriano, Elena
    Pudlo, Marc
    Luzet, Vincent
    Andrisano, Vincenza
    Jimeno, Maria-Luisa
    Lopez, Manuela G.
    Wehle, Sarah
    Gharbi, Tijani
    Refouvelet, Bernard
    de Andres, Lucia
    Herrera-Arozamena, Clara
    Monti, Barbara
    Bolognesi, Maria Laura
    Isabel Rodriguez-Franco, Maria
    Decker, Michael
    Marco-Contelles, Jose
    Ismaili, Lhassane
    CHEMMEDCHEM, 2015, 10 (03) : 523 - 539
  • [22] Selective ACAT Inhibitors as Promising Antihyperlipidemic, Antiatherosclerotic and Anti-Alzheimer Drugs
    Giovannoni, M. P.
    Dal Piaz, V.
    Vergelli, C.
    Barlocco, D.
    MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2003, 3 (06) : 576 - 584
  • [23] γ-Secretase Modulators as Potential Disease Modifying Anti-Alzheimer's Drugs
    Oehlrich, Daniel
    Berthelot, Didier J. -C.
    Gijsen, Harrie J. M.
    JOURNAL OF MEDICINAL CHEMISTRY, 2011, 54 (03) : 669 - 698
  • [24] Multifunctional neuroprotective derivatives of rasagiline as anti-alzheimer’s disease drugs
    Orly Weinreb
    Silvia Mandel
    Orit Bar-Am
    Merav Yogev-Falach
    Yael Avramovich-Tirosh
    Tamar Amit
    Moussa B. H. Youdim
    Neurotherapeutics, 2009, 6 : 163 - 174
  • [25] Multifunctional Neuroprotective Derivatives of Rasagiline as Anti-Alzheimer's Disease Drugs
    Weinreb, Orly
    Mandel, Silvia
    Bar-Am, Orit
    Yogev-Falach, Merav
    Avramovich-Tirosh, Yael
    Amit, Tamar
    Youdim, Moussa B. H.
    NEUROTHERAPEUTICS, 2009, 6 (01) : 163 - 174
  • [26] Genetics An anti-Alzheimer mutation
    Vernet, Agnes
    BIOFUTUR, 2012, (335) : 7 - 7
  • [27] Expanding the Multipotent Profile of Huprine-Tacrine Heterodimers as Disease-Modifying Anti-Alzheimer Agents
    Munoz-Torrero, Diego
    Pera, Marta
    Relat, Julia
    Ratia, Miriam
    Galdeano, Carles
    Viayna, Elisabet
    Sola, Irene
    Formosa, Xavier
    Camps, Pelayo
    Badia, Albert
    Victoria Clos, M.
    NEURODEGENERATIVE DISEASES, 2012, 10 (1-4) : 96 - 99
  • [28] Anti-alzheimer drugs in adults with Down's syndrome who are clinically dementing
    Brown, SW
    Mathurin, W
    McBrien, J
    Whitwham, S
    Masters, S
    JOURNAL OF NEUROLOGY NEUROSURGERY AND PSYCHIATRY, 2004, 75 (08): : 1220 - 1220
  • [29] Interaction between antidepressants and anti-Alzheimer drugs in modulating extrapyramidal side effects
    Shimizu, Saki
    Yamanaka, Megumi
    Inada, Akiyoshi
    Sogabe, Shunsaku
    Yanagisako, Ryoto
    Ohno, Yukihiro
    JOURNAL OF PHARMACOLOGICAL SCIENCES, 2016, 130 (03) : S160 - S160
  • [30] New anti-Alzheimer drugs from biodiversity: The role of the natural acetylcholinesterase inhibitors
    Viegas, C
    Bolzani, VD
    Barreiro, EJ
    Fraga, CAM
    MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2005, 5 (10) : 915 - 926