ArticleMolecules (Basel, Switzerland)2017
Synthesis of New Hydrazone Derivatives for MAO Enzymes Inhibitory Activity.
Article in Molecules (Basel, Switzerland), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
- Monoamine Oxidase Inhibitors in Drug Discovery Against Parkinson's Disease: An Update.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Inhibition of monoamine oxidases and neuroprotective effects: chalcones vs. chromones.Molecular diversity · 2025Article
- Novel Pyrrole Derivatives as Multi-Target Agents for the Treatment of Alzheimer's Disease: Microwave-Assisted Synthesis, In Silico Studies and Biological Evaluation.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Design, Synthesis, and Biological Effect Studies of Novel Benzofuran-Thiazolylhydrazone Derivatives as Monoamine Oxidase Inhibitors.ACS omega · 2024Article
- Synthesis, X-ray Structure, Hirshfeld, DFT Conformational, Cytotoxic, and Anti-Toxoplasma Studies of New Indole-Hydrazone Derivatives.International journal of molecular sciences · 2023Article
- Study on the Neuroprotective, Radical-Scavenging and MAO-B Inhibiting Properties of New Benzimidazole Arylhydrazones as Potential Multi-Target Drugs for the Treatment of Parkinson's Disease.Antioxidants (Basel, Switzerland) · 2022Article
- Inhibitory Potential of New Phenolic Hydrazide-Hydrazones with a Decoy Substrate Fragment towards Laccase from a Phytopathogenic Fungus: SAR and Molecular Docking Studies.International journal of molecular sciences · 2021Article
- Novel Thiosemicarbazone Derivatives: In Vitro and In Silico Evaluation as Potential MAO-B Inhibitors.Molecules (Basel, Switzerland) · 2021Article
- Coumarin-Chalcone Hybrids as Inhibitors of MAO-B: Biological Activity and In Silico Studies.Molecules (Basel, Switzerland) · 2021Article
- Synthesis,Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Design, Synthesis, In Vitro and In Silico Studies of New Thiazolylhydrazine-Piperazine Derivatives as Selective MAO-A Inhibitors.Molecules (Basel, Switzerland) · 2020Article
- Article
- Synthesis and Structure-Activity Relationship Studies of Hydrazide-Hydrazones as Inhibitors of Laccase fromMolecules (Basel, Switzerland) · 2020Article
- Synthesis and AChE Inhibitory Activity of Novel Thiazolylhydrazone Derivatives.Molecules (Basel, Switzerland) · 2019Article
- Synthesis of New Benzothiazole Acylhydrazones as Anticancer Agents.Molecules (Basel, Switzerland) · 2018Article
- Design, Synthesis and Biological Evaluation of Novel N-Pyridyl-Hydrazone Derivatives as Potential Monoamine Oxidase (MAO) Inhibitors.Molecules (Basel, Switzerland) · 2018Article
- Design and Synthesis of New Benzothiazole Compounds as Selective hMAO-B Inhibitors.Molecules (Basel, Switzerland) · 2017Article
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8 authors.
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Abstract
In the present work, 14 new 1-substituted-2-phenylhydrazone derivatives were synthesized to evaluate their inhibitory activity against hMAO enzymes. The structures of the newly synthesized hydrazones 2a-2n were characterized by IR, 1H-NMR, 13C-NMR, HR-MS spectroscopic methods. The inhibitory activity of compounds 2a-2n against hMAO-A and hMAO-B enzymes was elucidated by using an in-vitro Amplex Red® reagent assay based on fluorometric methods. According to the activity studies, 2a and 2b were found to be the most active compounds against hMAO-A enzyme, with IC50 values of 0.342 µM and 0.028 µM, respectively. The most active compounds 2a-2b were evaluated by means of enzyme kinetics and docking studies. Moreover, these compounds were subjected to cytotoxicity and genotoxicity tests to establish their preliminary toxicological profiles and were found to be non-cytotoxic and non-genotoxic. Consequently, the findings of this study display the biological importance of compounds 2a, 2b as selective, irreversible and competitive inhibitors of hMAO-A. Docking studies revealed that there is a strong interaction between hMAO-A and the most active compound 2b.
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