scholarly journals Design, Synthesis and in vitro Evaluation of Indolotacrine Analogues as Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease

ChemMedChem ◽  
2015 ◽  
Vol 11 (12) ◽  
pp. 1264-1269 ◽  
Author(s):  
Ondrej Benek ◽  
Ondrej Soukup ◽  
Marketa Pasdiorova ◽  
Lukas Hroch ◽  
Vendula Sepsova ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Design Synthesis ◽  
In Vitro Evaluation

scholarly journals Design, synthesis, structure, toxicology and in vitro testing of three novel agents for Alzheimer’s disease

RSC Advances ◽  
2017 ◽  
Vol 7 (38) ◽  
pp. 23457-23467 ◽  
Author(s):  
José Daniel Figueroa-Villar
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Novel Agents ◽  
In Vitro Testing ◽  
Design Synthesis

This article describes the synthesis of three novel compounds for the treatment of Alzheimer’s disease (AD).

scholarly journals Design, Synthesis, and In Vitro Evaluation of Hydroxybenzimidazole-Donepezil Analogues as Multitarget-Directed Ligands for the Treatment of Alzheimer’s Disease

Molecules ◽  
2020 ◽  
Vol 25 (4) ◽  
pp. 985 ◽  
Author(s):  
Sílvia Chaves ◽  
Simonetta Resta ◽  
Federica Rinaldo ◽  
Marina Costa ◽  
Romane Josselin ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Neuroblastoma Cells ◽  
Biological Properties ◽  
Design Synthesis ◽  
Aβ Aggregation ◽  
Structural Isomerization ◽  
Good Potential ◽  
Nitro Derivatives

A series of multi-target-directed ligands (MTDLs), obtained by attachment of a hydroxyphenylbenzimidazole (BIM) unit to donepezil (DNP) active mimetic moiety (benzyl-piperidine/-piperazine) was designed, synthesized, and evaluated as potential anti-Alzheimer’s disease (AD) drugs in terms of biological activity (inhibition of acetylcholinesterase (AChE) and β–amyloid (Aβ) aggregation), metal chelation, and neuroprotection capacity. Among the DNP-BIM hybrids studied herein, the structural isomerization did not significantly improve the biological properties, while some substitutions, namely fluorine atom in each moiety or the methoxy group in the benzyl ring, evidenced higher cholinergic AChE activity. All the compounds are able to chelate Cu and Zn metal ions through their bidentate BIM moieties, but compound 5, containing a three-dentate chelating unit, is the strongest Cu(II) chelator. Concerning the viability on neuroblastoma cells, compounds 9 and 10 displayed the highest reduction of Aβ-induced cell toxicity. In silico calculations of some pharmacokinetic descriptors indicate that all the compounds but the nitro derivatives have good potential oral-bioavailability. Overall, it can be concluded that most of the studied DNP-BIM conjugates showed quite good anti-AD properties, therefore deserving to be considered in further studies with the aim of understanding and treating AD.

[P1-039]: IN VITRO EVALUATION OF BENZOTHIAZOLE-BASED UREAS AS POTENTIAL ABAD/17β-HSD10 MODULATORS FOR ALZHEIMER'S DISEASE THERAPEUTICS

2017 ◽  
Vol 13 (7S_Part_5) ◽  
pp. P249-P249 ◽  
Author(s):  
Laura Aitken ◽  
Lukas Hroch ◽  
Rebecca Hughes ◽  
Thijs S. Udo ◽  
Ondrej Benek ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
In Vitro Evaluation

Synthesis, in vitro evaluation and molecular docking of a new class of indolylpropyl benzamidopiperazines as dual AChE and SERT ligands for Alzheimer’s disease

2020 ◽  
Vol 198 ◽  
pp. 112368 ◽  
Author(s):  
Julio Rodríguez-Lavado ◽  
Carlos Gallardo-Garrido ◽  
Michael Mallea ◽  
Victor Bustos ◽  
Rodrigo Osorio ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Molecular Docking ◽  
In Vitro Evaluation ◽  
New Class

scholarly journals Design, synthesis, in vitro and in vivo evaluation of tacrine–cinnamic acid hybrids as multi-target acetyl- and butyrylcholinesterase inhibitors against Alzheimer's disease

RSC Advances ◽  
2017 ◽  
Vol 7 (54) ◽  
pp. 33851-33867 ◽  
Author(s):  
Yao Chen ◽  
Hongzhi Lin ◽  
Jie Zhu ◽  
Kai Gu ◽  
Qi Li ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cinnamic Acid ◽  
Cholinesterase Inhibitors ◽  
In Vivo Evaluation ◽  
Design Synthesis

A series of tacrine–cinnamic acid hybrids are synthesized as multi-target cholinesterase inhibitors against Alzheimer's disease.

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