ArticleDrug design, development and therapy2020
Reversible Small Molecule Inhibitors of MAO A and MAO B with Anilide Motifs.
Article in Drug design, development and therapy, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- Article
- Probing the inhibition of MAO-B by chalcones: an integrated approach combining molecular docking, ADME analysis, MD simulation, and MM-PBSA calculations.Journal of molecular modeling · 2024Article
- Article
- Quantitative Structure-Neurotoxicity Assessment and In Vitro Evaluation of Neuroprotective and MAO-B Inhibitory Activities of SeriesMolecules (Basel, Switzerland) · 2022Article
- Design, Synthesis, and Biological Evaluation of Novel MAO-A Inhibitors Targeting Lung Cancer.Molecules (Basel, Switzerland) · 2022Article
- Replacement of Chalcone-Ethers with Chalcone-Thioethers as Potent and Highly Selective Monoamine Oxidase-B Inhibitors and Their Protein-Ligand Interactions.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Novel Thiosemicarbazone Derivatives: In Vitro and In Silico Evaluation as Potential MAO-B Inhibitors.Molecules (Basel, Switzerland) · 2021Article
- Development of Halogenated Pyrazolines as Selective Monoamine Oxidase-B Inhibitors: Deciphering via Molecular Dynamics Approach.Molecules (Basel, Switzerland) · 2021Article
- Design, Synthesis, and Biological Evaluation of Pyridazinones Containing the (2-Fluorophenyl) Piperazine Moiety as Selective MAO-B Inhibitors.Molecules (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
7 authors.
Funding
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Abstract
backgroundLigands consisting of two aryl moieties connected via a short spacer were shown to be potent inhibitors of monoamine oxidases (MAO) A and B, which are known as suitable targets in treatment of neurological diseases. Based on this general blueprint, we synthesized a series of 66 small aromatic amide derivatives as novel MAO A/B inhibitors.
methodsThe compounds were synthesized, purified and structurally confirmed by spectroscopic methods. Fluorimetric enzymological assays were performed to determine MAO A/B inhibition properties. Mode and reversibility of inhibition was determined for the most potent MAO B inhibitor. Docking poses and pharmacophore models were generated to confirm the in vitro results.
results
conclusionThe small molecule anilides with different substitution patterns were identified as potent MAO A/B inhibitors, which were active in nanomolar concentrations ranges. These small and easily accessible molecules are promising motifs, especially for newly designed multitargeted ligands taking advantage of these fragments.
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