Novel tacrine-scutellarin hybrids as multipotent anti-Alzheimer's agents: Design, synthesis and biological evaluation

K Spilovska, J Korabecny, V Sepsova, D Jun… - Molecules, 2017 - mdpi.com
A novel series of 6-chlorotacrine-scutellarin hybrids was designed, synthesized and the
biological activity as potential anti-Alzheimer's agents was assessed. Their inhibitory activity …

Chlorinated tacrine analogs: Design, synthesis and biological evaluation of their anti-cholinesterase activity as potential treatment for Alzheimer's disease

HM Ragab, M Teleb, HR Haidar, N Gouda - Bioorganic chemistry, 2019 - Elsevier
In search of potent acetyl cholinesterase inhibitors with low hepatotoxicity for the treatment of
Alzheimer's disease, introduction of a chloro substitution to tacrine and some of its analogs …

[HTML][HTML] Multi-target-directed therapeutic potential of 7-methoxytacrine-adamantylamine heterodimers in the Alzheimer's disease treatment

Z Gazova, O Soukup, V Sepsova, K Siposova… - … et Biophysica Acta (BBA …, 2017 - Elsevier
Alzheimer's disease (AD) is a progressive neurodegenerative disorder and currently there is
no efficient treatment. The classic drug-design strategy based on the “one-molecule-one …

Novel series of tacrine-tianeptine hybrids: Synthesis, cholinesterase inhibitory activity, S100B secretion and a molecular modeling approach

MA Ceschi, JS da Costa, JPB Lopes… - European Journal of …, 2016 - Elsevier
Tianeptine was linked to various 9-aminoalkylamino-1, 2, 3, 4-tetrahydroacridines using
EDC· HCl/HOBt to afford a series of tacrine-tianeptine hybrids. The hybrids were tested for …

Phenothiazine-Tacrine Heterodimers: Pursuing Multitarget Directed Approach in Alzheimer's Disease

L Gorecki, E Uliassi, M Bartolini… - ACS Chemical …, 2021 - ACS Publications
Since 2002, no clinical candidate against Alzheimer's disease has reached the market;
hence, an effective therapy is urgently needed. We followed the so-called “multitarget …

Exploring structure-activity relationship in tacrine-squaramide derivatives as potent cholinesterase inhibitors

B Svobodova, E Mezeiova, V Hepnarova, M Hrabinova… - Biomolecules, 2019 - mdpi.com
Tacrine was the first drug to be approved for Alzheimer's disease (AD) treatment, acting as a
cholinesterase inhibitor. The neuropathological hallmarks of AD are amyloid-rich senile …

Design, synthesis and evaluation of OA-tacrine hybrids as cholinesterase inhibitors with low neurotoxicity and hepatotoxicity against Alzheimer's disease

H Yang, H Jia, M Deng, K Zhang, Y Liu… - Journal of Enzyme …, 2023 - Taylor & Francis
A series of OA-tacrine hybrids with the alkylamine linker was designed, synthesized, and
evaluated as effective cholinesterase inhibitors for the treatment of Alzheimer's disease …

Synthesis, biological evaluation and modeling of hybrids from tetrahydro-1H-pyrazolo [3, 4-b] quinolines as dual cholinestrase and COX-2 inhibitors

M Mroueh, WH Faour, WN Shebaby, CF Daher… - Bioorganic …, 2020 - Elsevier
Abstract New tetrahydro-1H-pyrazolo [3, 4-b] quinoline derivatives were designed,
synthesized and characterized as dual anticholinestrase and cyclooxygenase-2 inhibitors …

Cholinesterase inhibitor 6-chlorotacrine-In vivo toxicological profile and behavioural effects

J Misik, E Nepovimova, J Pejchal… - Current Alzheimer …, 2018 - ingentaconnect.com
Background: 6-chlorotacrine is a cholinesterase inhibitor showing good inhibitory potential,
even better than parent compound tacrine, in vitro. Despite tacrine scaffold is broadly used …

7-Methoxytacrine-p-Anisidine Hybrids as Novel Dual Binding Site Acetylcholinesterase Inhibitors for Alzheimer's Disease Treatment

J Korabecny, M Andrs, E Nepovimova, R Dolezal… - Molecules, 2015 - mdpi.com
Alzheimer's disease (AD) is a debilitating progressive neurodegenerative disorder that
ultimately leads to the patient's death. Despite the fact that novel pharmacological …