Assessing Cholinesterase Inhibitors

Te lecture presents modern concept of the symptoms, diagnosis and treatment of dementia with Lewy bodies (DLB), which accounts for about 10% of cases of dementia. Te nosological status of DLB and the problem of ratio of DLB and Parkinson’s disease which, apparently, represent two phenotypic variants of one neurodegenerative process («diseases with Lewy bodies») are considered in historical aspect. Approaches to the diagnosis and coding of DLB in accordance with ICD-10 are proposed. Te role of cholinesterase inhibitors, antipsychotics, levodopa, rasagiline and other drugs in the treatment of patients with DLB is аnalyzed.

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Faculty Opinions recommendation of Syncope and its consequences in patients with dementia receiving cholinesterase inhibitors: a population-based cohort study.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1836966.1378067 ◽

2010 ◽

Author(s):

Kirk Daffner

Keyword(s):

Cohort Study ◽

Cholinesterase Inhibitors ◽

Population Based

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Rationale for the Development of Cholinesterase Inhibitors as Anti- Alzheimer Agents

Current Pharmaceutical Design ◽

10.2174/1381612043383331 ◽

2004 ◽

Vol 10 (25) ◽

pp. 3111-3119 ◽

Cited By ~ 52

Author(s):

D. Lahiri ◽

J. Rogers ◽

N. Greig ◽

K. Sambamurti

Keyword(s):

Cholinesterase Inhibitors

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Recent Knowledge on Medicinal Plants as Source of Cholinesterase Inhibitors for the Treatment of Dementia

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557515666150709104731 ◽

2016 ◽

Vol 16 (8) ◽

pp. 605-618 ◽

Cited By ~ 13

Author(s):

Rosa Tundis ◽

Marco Bonesi ◽

Francesco Menichini ◽

Monica R. Loizzo

Keyword(s):

Medicinal Plants ◽

Cholinesterase Inhibitors

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Drug Design of Inhibitors of Alzheimer’s Disease (AD): POM and DFT Analyses of Cholinesterase Inhibitory Activity of β-amino di-Carbonyl Derivatives

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557518666181102102816 ◽

2019 ◽

Vol 19 (8) ◽

pp. 688-705

Author(s):

Taibi Ben Hadda ◽

Abdur Rauf ◽

Hsaine Zgou ◽

Fatma Sezer Senol ◽

Ilkay Erdogan Orhan ◽

...

Keyword(s):

Alzheimer’S Disease ◽

Alzheimer's Disease ◽

Cholinesterase Inhibitors ◽

Metal Accumulation ◽

Microtiter Plate ◽

Metal Chelation ◽

Carbonyl Derivatives ◽

Cholinesterase Inhibitory Activity ◽

Inhibitory Potential

Background:Since deficit of acetylcholine has been evidenced in the Alzheimer’s disease (AD) patients, cholinesterase inhibitors are currently the most specified drug category for the remediation of AD.Method:In the present study, 16 compounds (1-16) with dicarbonyl skeletons have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 100 μg/mL. Since metal accumulation is related to AD, the compounds were also tested for their metal-chelation capacity.Results and Conclusion:All the investigated dicarbonyl compounds exerted none or lower than 30% inhibition against both cholinesterases, whereas compounds 2, 8 and 11 showed 37, 42, 41% of inhibition towards BChE, being the most active. The highest metal-chelation capacity was observed with compound 8 (53.58 ± 2.06%). POM and DFT analyses are in good harmonization with experimental data.

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Inhibitors of Cholinesterases in Pharmacology: the Current Trends

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557519666191018170908 ◽

2020 ◽

Vol 20 (15) ◽

pp. 1532-1542 ◽

Cited By ~ 1

Author(s):

Miroslav Pohanka

Keyword(s):

Molecular Weight ◽

Cholinesterase Inhibitors ◽

Recent Literature ◽

Nerve Agents ◽

Low Molecular Weight ◽

Toxic Compounds ◽

Current Trends ◽

Low Molecular Weight Compounds ◽

Wide Group ◽

Anti Inflammation

Inhibitors of cholinesterases are a wide group of low molecular weight compounds with a significant role in the current pharmacology. Besides the pharmacological importance, they are also known as toxic compounds like military nerve agents. In the pharmacology, drugs for Alzheimer disease, myasthenia gravis and prophylaxis of poisoning by nerve agents can be mentioned as the relevant applications. Besides this, anti-inflammation and antiphrastic drugs are other pharmacological applications of these inhibitors. This review is focused on a survey of cholinesterase inhibitors with known or expected pharmacological impact and indications of their use. Recent literature with comments is provided here as well.

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