ArticleMolecules (Basel, Switzerland)2012
Acetylcholinesterase-inhibiting activity of salicylanilide N-alkylcarbamates and their molecular docking.
Article in Molecules (Basel, Switzerland), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 53 citations in OpenAlex.
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- In Silico and In Vitro Studies of Benzothiazole-Isothioureas Derivatives as a Multitarget Compound for Alzheimer's Disease.International journal of molecular sciences · 2022Article
- Study of Biological Activities and ADMET-Related Properties of Salicylanilide-Based Peptidomimetics.International journal of molecular sciences · 2022Article
- Study of Biological Activities and ADMET-Related Properties of Novel ChlorinatedInternational journal of molecular sciences · 2022Article
- New 3-Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Novel Sulfonamide-Based Carbamates as Selective Inhibitors of BChE.International journal of molecular sciences · 2021Article
- Synthesis and Hybrid SAR Property Modeling of Novel Cholinesterase Inhibitors.International journal of molecular sciences · 2021Article
- Therapeutic Potential of Multifunctional Derivatives of Cholinesterase Inhibitors.Current neuropharmacology · 2021Article
- Acetylcholinesterase inhibition in electric eel and human donor blood: an in vitro approach to investigate interspecies differences and human variability in toxicodynamics.Archives of toxicology · 2020Article
- Article
- Novel Benzene-Based Carbamates for AChE/BChE Inhibition: Synthesis and Ligand/Structure-Oriented SAR Study.International journal of molecular sciences · 2019Article
- Therapeutic potency of substituted chromones as Alzheimer's drug: Elucidation of acetylcholinesterase inhibitory activity through spectroscopic and molecular modelling investigation.BioImpacts : BI · 2019Article
- Metformin and its sulphonamide derivative simultaneously potentiateanti-cholinesterase activity of donepezil and inhibit beta-amyloid aggregation.Journal of enzyme inhibition and medicinal chemistry · 2018Article
- Metformin - a Future Therapy for Neurodegenerative Diseases : Theme: Drug Discovery, Development and Delivery in Alzheimer's Disease Guest Editor: Davide Brambilla.Pharmaceutical research · 2017Review
- Proline-Based Carbamates as Cholinesterase Inhibitors.Molecules (Basel, Switzerland) · 2017Article
- Metformin and Its Sulfenamide Prodrugs Inhibit Human Cholinesterase Activity.Oxidative medicine and cellular longevity · 2017Article
- Novel Cholinesterase Inhibitors Based on O-Aromatic N,N-Disubstituted Carbamates and Thiocarbamates.Molecules (Basel, Switzerland) · 2016Article
- In vitro bactericidal activity of 4- and 5-chloro-2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides against MRSA.BioMed research international · 2015Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A series of twenty-five novel salicylanilide N-alkylcarbamates were investigated as potential acetylcholinesterase inhibitors. The compounds were tested for their ability to inhibit acetylcholinesterase (AChE) from electric eel (Electrophorus electricus L.). Experimental lipophilicity was determined, and the structure-activity relationships are discussed. The mode of binding in the active site of AChE was investigated by molecular docking. All the discussed compounds expressed significantly higher AChE inhibitory activity than rivastigmine and slightly lower than galanthamine. Disubstitution by chlorine in C'(₃,₄) of the aniline ring and the optimal length of hexyl-undecyl alkyl chains in the carbamate moiety provided the most active AChE inhibitors. Monochlorination in C'(₄) exhibited slightly more effective AChE inhibitors than in C'(₃). Generally it can be stated that compounds with higher lipophilicity showed higher inhibition, and the activity of the compounds is strongly dependent on the length of the N-alkyl chain.
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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.