ArticlePloS one2018
Design and evaluation of selective butyrylcholinesterase inhibitors based on Cinchona alkaloid scaffold.
Article in PloS one, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 31 citations in OpenAlex.
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- Evaluation of the Key Structural Features of Various Butyrylcholinesterase Inhibitors Using Simple Molecular Descriptors.Molecules (Basel, Switzerland) · 2022Article
- Design, Synthesis and Biological Evaluation of Biscarbamates as Potential Selective Butyrylcholinesterase Inhibitors for the Treatment of Alzheimer's Disease.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Synthesis, Biological Evaluation and Machine Learning Prediction Model for FluorinatedPharmaceuticals (Basel, Switzerland) · 2022Article
- Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model.RSC medicinal chemistry · 2022Article
- 4-Aminoquinoline-Based Adamantanes as Potential Anticholinesterase Agents in Symptomatic Treatment of Alzheimer's Disease.Pharmaceutics · 2022Article
- Mechanistic interplay of various mediators involved in mediating the neuroprotective effect of daphnetin.Pharmacological reports : PR · 2021Review
- Selective BuChE Inhibitory Activity, Chemical Composition, and Enantiomeric Content of the Essential Oil fromPlants (Basel, Switzerland) · 2021Article
- Antimicrobial Activity of Quasi-EnantiomericAntibiotics (Basel, Switzerland) · 2021Article
- Chemical Composition and Anticholinesterase Activity of the Essential Oil of Leaves and Flowers from the Ecuadorian PlantMolecules (Basel, Switzerland) · 2021Article
- Quinuclidine-Based Carbamates as Potential CNS Active Compounds.Pharmaceutics · 2021Article
- Design, synthesis and cholinesterase inhibitory properties of new oxazole benzylamine derivatives.Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Vitamin B3-Based Biologically Active Compounds as Inhibitors of Human Cholinesterases.International journal of molecular sciences · 2020Article
- Benzobicyclo[3.2.1]octene Derivatives as a New Class of Cholinesterase Inhibitors.Molecules (Basel, Switzerland) · 2020Article
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
This paper describes the synthesis and anticholinesterase potency of Cinchona-based alkaloids; ten quaternary derivatives of cinchonines and their corresponding pseudo-enantiomeric cinchonidines. The quaternization of quinuclidine moiety of each compound was carried out with groups diverse in their size: methyl, benzyl and differently meta- and para-substituted benzyl groups. All of the prepared compounds reversibly inhibited human butyrylcholinesterase and acetylcholinesterase with Ki constants within nanomolar to micromolar range. Five cinchonidine derivatives displayed 95-510 times higher inhibition selectivity to butyrylcholinesterase over acetylcholinesterase and four were potent butyrylcholinesterase inhibitors with Ki constants up to 100 nM, of which N-para-bromobenzyl cinchonidinium bromide can be considered a lead for further modifications and optimizations for possible use in the treatment of neurodegenerative diseases.
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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.