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).

Design, synthesis and in vitro testing of 7-methoxytacrine-amantadine analogues: a novel cholinesterase inhibitors for the treatment of Alzheimer’s disease

2015 ◽  
Vol 24 (6) ◽  
pp. 2645-2655 ◽  
Author(s):  
Katarina Spilovska ◽  
Jan Korabecny ◽  
Anna Horova ◽  
Kamil Musilek ◽  
Eugenie Nepovimova ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitors ◽  
In Vitro Testing ◽  
Design Synthesis

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.

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, 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.

Acetylcholinesterase Inhibitory Potential and Antioxidant Activities of Five Cultivars of Rosa Damascena Mill. From Isparta, Turkey

2020 ◽  
Vol 18 (4) ◽  
pp. 354-359
Author(s):  
Shirin Tarbiat ◽  
Azize Simay Türütoğlu ◽  
Merve Ekingen
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Free Radical ◽  
Neurodegenerative Disorder ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Acetylcholinesterase Activity ◽  
Rosa Damascena ◽  
Free Radical Damage

Alzheimer's disease is a neurodegenerative disorder characterized by memory loss and impairment of language. Alzheimer's disease is strongly associated with oxidative stress and impairment in the cholinergic pathway, which results in decreased levels of acetylcholine in certain areas of the brain. Hence, inhibition of acetylcholinesterase activity has been recognized as an acceptable treatment against Alzheimer's disease. Nature provides an array of bioactive compounds, which may protect against free radical damage and inhibit acetylcholinesterase activity. This study compares the in vitro antioxidant and anticholinesterase activities of hydroalcoholic extracts of five cultivars of Rosa Damascena Mill. petals (R. damascena 'Bulgarica', R. damascena 'Faik', R. damascena 'Iranica', R. damascena 'Complex-635' and R. damascena 'Complex-637') from Isparta, Turkey. The antioxidant activities of the hydroalcoholic extracts were tested for ferric ion reduction and DPPH radical scavenging activities. The anti-acetylcholinesterase activity was also evaluated. All rose cultivars showed a high potency for scavenging free radical and inhibiting acetylcholinesterase activity. There was a significant correlation between antioxidant and acetylcholinesterase inhibitory activity. Among cultivars, Complex-635 showed the highest inhibitory effect with an IC50 value of 3.92 µg/mL. Our results suggest that all these extracts may have the potential to treat Alzheimer's disease with Complex-635 showing more promise.

Sign in / Sign up

Export Citation Format

Share Document