Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease

J Jeřábek, E Uliassi, L Guidotti, J Korábečný… - European Journal of …, 2017 - Elsevier
Multi-target drug discovery is one of the most followed approaches in the active central
nervous system (CNS) therapeutic area, especially in the search for new drugs against …

SAR study to find optimal cholinesterase reactivator against organophosphorous nerve agents and pesticides

L Gorecki, J Korabecny, K Musilek, D Malinak… - Archives of …, 2016 - Springer
Irreversible inhibition of acetylcholinesterase (AChE) by organophosphates leads to many
failures in living organism and ultimately in death. Organophosphorus compounds …

Synthesis and anticholinesterase activity of coumarin-3-carboxamides bearing tryptamine moiety

S Ghanei-Nasab, M Khoobi, F Hadizadeh… - European journal of …, 2016 - Elsevier
Abstract A number of N-(2-(1H-indol-3-yl) ethyl)-2-oxo-2H-chromene-3-carboxamides were
synthesized and tested against AChE and BuChE. The in vitro assessment of the …

Multitarget tacrine hybrids with neuroprotective properties to confront Alzheimer's disease

K Spilovska, J Korabecny… - Current Topics in …, 2017 - ingentaconnect.com
Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder. Several hallmarks
such as β-amyloid (Aβ) aggregation underlying amyloid plaque formation, Τ …

Technological solutions for older people with Alzheimer's disease

P Maresova, S Tomsone, P Lameski… - Current Alzheimer …, 2018 - ingentaconnect.com
In the nineties, numerous studies began to highlight the problem of the increasing number of
people with Alzheimer's disease in developed countries, especially in the context of …

Design, synthesis and biological evaluation of novel donepezil–coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease

SS Xie, JS Lan, X Wang, ZM Wang, N Jiang, F Li… - Bioorganic & Medicinal …, 2016 - Elsevier
Combining N-benzylpiperidine moiety of donepezil and coumarin into in a single molecule,
novel hybrids with ChE and MAO-B inhibitory activity were designed and synthesized. The …

Progress in drug development for Alzheimer's disease: An overview in relation to mitochondrial energy metabolism

J Hroudová, N Singh, Z Fišar, KK Ghosh - European journal of medicinal …, 2016 - Elsevier
Current possibilities of Alzheimer's disease (AD) treatment are very limited and are based on
administration of cholinesterase inhibitors (donepezil, rivastigmine, galantamine) and/or N …

The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease

V Hepnarova, J Korabecny, L Matouskova… - European Journal of …, 2018 - Elsevier
Novel tacrine-benzyl quinolone carboxylic acid (tacrine-BQCA) hybrids were designed
based on multi-target directed ligands (MTLDs) paradigm, synthesized and evaluated in …

7-MEOTA–donepezil like compounds as cholinesterase inhibitors: Synthesis, pharmacological evaluation, molecular modeling and QSAR studies

J Korabecny, R Dolezal, P Cabelova, A Horova… - European journal of …, 2014 - Elsevier
A novel series of 7-methoxytacrine (7-MEOTA)–donepezil like compounds was synthesized
and tested for their ability to inhibit electric eel acetylcholinesterase (EeAChE), human …

Tacrine first-phase biotransformation and associated hepatotoxicity: a possible way to avoid quinone methide formation

M Novak, M Vajrychova, S Koutsilieri… - ACS Chemical …, 2023 - ACS Publications
Tacrine was withdrawn from clinical use as a drug against Alzheimer's disease in 2013,
mainly due to drug-induced liver injury. The culprit of tacrine-associated hepatotoxicity is …