Evidence map›Paper›PMID 36297332›Full record

ArticlePharmaceuticals (Basel, Switzerland)2022

Design, Synthesis and Biological Evaluation of Biscarbamates as Potential Selective Butyrylcholinesterase Inhibitors for the Treatment of Alzheimer's Disease.

Ana Matošević, Anamarija Knežević, Antonio Zandona, Nikola Maraković, Zrinka Kovarik, Anita Bosak

Abstract read
In one paragraph

Article in Pharmaceuticals (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

9 citing papers in PubMed.

  1. Article
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  5. Evaluation of hydrazone andJournal of enzyme inhibition and medicinal chemistry · 2024
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors.

Ana MatoševićBiochemistry and Organic Analytical Chemistry Unit, Institute for Medical Research and Occupational Health, HR-10000 Zagreb, Croatia.
Anamarija KneževićDivision of Organic Chemistry and Biochemistry, Ruđer Bošković Institute, HR-10000 Zagreb, Croatia.ORCID 0000-0003-3736-912X
Antonio ZandonaBiochemistry and Organic Analytical Chemistry Unit, Institute for Medical Research and Occupational Health, HR-10000 Zagreb, Croatia.ORCID 0000-0002-3937-3520
Nikola MarakovićBiochemistry and Organic Analytical Chemistry Unit, Institute for Medical Research and Occupational Health, HR-10000 Zagreb, Croatia.
Zrinka KovarikBiochemistry and Organic Analytical Chemistry Unit, Institute for Medical Research and Occupational Health, HR-10000 Zagreb, Croatia.ORCID 0000-0001-9863-886X
Anita BosakBiochemistry and Organic Analytical Chemistry Unit, Institute for Medical Research and Occupational Health, HR-10000 Zagreb, Croatia.ORCID 0000-0003-0164-4994

Funding

Croatian Science Foundation IP-2018-01-7683, IP-2020-02-9343
6 · The paper itself

Abstract

As butyrylcholinesterase (BChE) plays a role in the progression of symptoms and pathophysiology of Alzheimer's disease (AD), selective inhibition of BChE over acetylcholinesterase (AChE) can represent a promising pathway in treating AD. The carbamate group was chosen as a pharmacophore because the carbamates currently or previously in use for the treatment of AD displayed significant positive effects on cognitive symptoms. Eighteen biscarbamates with different substituents at the carbamoyl and hydroxyaminoethyl chain were synthesized, and their inhibitory potential toward both cholinesterases and inhibition selectivity were determined. The ability of carbamates to cross the blood-brain barrier (BBB) by passive transport, their cytotoxic profile and their ability to chelate biometals were also evaluated. All biscarbamates displayed a time-dependent inhibition with inhibition rate constants within 10

Indexed as

acetylcholinesterasedetailed kinetic studymetal chelatingmolecular dockingrate constantsspontaneous decarbamylation

Identifiers

PMID36297332
PMCPMC9609992

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.