ArticleJournal of enzyme inhibition and medicinal chemistry2019
4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis.
Article in Journal of enzyme inhibition and medicinal chemistry, 2019. 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.
- Monoamine Oxidase Inhibitors in Drug Discovery Against Parkinson's Disease: An Update.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Using computer modeling to find new LRRK2 inhibitors for parkinson's disease.Scientific reports · 2025Article
- Targeting MAO-B with Small-Molecule Inhibitors: A Decade of Advances in Anticancer Research (2012-2024).Molecules (Basel, Switzerland) · 2024Review
- Machine learning accelerates pharmacophore-based virtual screening of MAO inhibitors.Scientific reports · 2024Article
- Computational Chemistry and Molecular Modeling of Reversible MAO Inhibitors.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Synthesis of Novel Aminothiazole Derivatives as Promising Antiviral, Antioxidant and Antibacterial Candidates.International journal of molecular sciences · 2022Article
- The Diverse Biological Activity of Recently Synthesized Nitro Compounds.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Morpholine-based chalcones as dual-acting monoamine oxidase-B and acetylcholinesterase inhibitors: synthesis and biochemical investigations.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Evaluation of the combined activity of benzimidazole arylhydrazones as new anti-Parkinsonian agents: monoamine oxidase-B inhibition, neuroprotection and oxidative stress modulation.Neural regeneration research · 2021Article
- Cyclopentanone Derivative Attenuates Memory Impairment by Inhibiting Amyloid Plaques Formation in the 5xFAD Mice.International journal of molecular sciences · 2021Article
- Recent Developments in New Therapeutic Agents against Alzheimer and Parkinson Diseases: In-Silico Approaches.Molecules (Basel, Switzerland) · 2021Review
- Antitumor properties of certain spirooxindoles towards hepatocellular carcinoma endowed with antioxidant activity.Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Attenuation of Spatial Memory in 5xFAD Mice by Halting Cholinesterases, Oxidative Stress and Neuroinflammation Using a Cyclopentanone Derivative.Pharmaceuticals (Basel, Switzerland) · 2020Article
- Benzo[Journal of enzyme inhibition and medicinal chemistry · 2019Article
- The Up-Regulation of Oxidative Stress as a Potential Mechanism of Novel MAO-B Inhibitors for Glioblastoma Treatment.Molecules (Basel, Switzerland) · 2019Article
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11 authors.
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Abstract
A new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesised, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted (hetero)aromatic substituents were linked to N1 of the hydrazone in order to establish robust structure-activity relationships. The results of the biological testing demonstrated that the presence of the hydrazothiazole nucleus bearing at C4 a phenyl ring functionalised at the meta position with a nitro group represents an important pharmacophoric feature to obtain selective and reversible human MAO-B inhibition for the treatment of neurodegenerative disorders. In addition, the most potent and selective MAO-B inhibitors were evaluated in silico as potential cholinesterase (AChE/BuChE) inhibitors and in vitro for antioxidant activities. The results obtained from molecular modelling studies provided insight into the multiple interactions and structural requirements for the reported MAO inhibitory properties.
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