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Design, synthesis, docking studies and monoamine oxidase inhibition of a small library of 1-acetyl- and 1-thiocarbamoyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazoles
(MDPI, 2019)
New N-acetyl/N-thiocarbamoylpyrazoline derivatives were designed and synthesized
in high yields to assess their inhibitory activity and selectivity against human monoamine oxidase
A and B. The most important chiral ...
4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis
(Taylor & Francis, 2019)
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 ...
Benzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activity
(Taylor & Francis, 2019)
A series of benzo[b]thiophen-3-ols were synthesised and investigated as potential human monoamine oxidase (hMAO) inhibitors in vitro as well as ex vivo in rat cortex synaptosomes by means of evaluation of 3,4-dihydroxyphenylacetic ...
Synthesis and evaluation of chromone derivatives as inhibitors of monoamine oxidase
(Springer, 2019)
Based on reports that chromone compounds are good potency inhibitors of monoamine oxidase (MAO), the present study evaluates the effect of substitution with flexible side chains on the 3 position on MAO inhibition potency. ...
SAR and molecular mechanism studies of monoamine oxidase inhibition by selected chalcone analogs
(Taylor & Francis, 2019)
The present study describes the synthesis of a series of 22 chalcone analogs. These compounds were evaluated as potential human MAO-A and MAO-B inhibitors. The compounds showed varied selectivity against the two isoforms. ...
Evaluation of selected natural compounds as dual inhibitors of catechol-o-methyltransferase and monoamine oxidase
(Bentham Science, 2019)
Background: The most effective symptomatic treatment of Parkinson’s disease remains the metabolic precursor of dopamine, L-dopa. To enhance the efficacy of L-dopa, it is often combined with inhibitors of the enzymes, ...
The monoamine oxidase inhibition properties of C6-mono- and N3/C6-disubstituted derivatives of 4(3H)-quinazolinone
(Elsevier, 2019)
Parkinson’s disease is characterised by the death of the nigrostriatal neurons and depletion of striatal dopamine. The standard symptomatic therapy consists of dopamine replacement with l-dopa, the metabolic precursor of ...
Novel monoamine oxidase inhibitors based on the privileged 2-imidazoline molecular framework
(Elsevier, 2019)
Series of structurally diverse 2-imidazoline derivatives have been synthesized by condensation of substituted aldehydes with ethylenediamine, Pd-catalyzed N-arylation of 2-imidazolines and by the formation of 1,2,4-oxadiazoles ...
Monoamine oxidase inhibition by selected dye compounds
(Wiley, 2019)
Monoamine oxidase (MAO) is an important drug target as the MAO isoforms play key roles in neurodegenerative disorders such as Alzheimer's disease and Parkinson's disease, as well as in neuropsychiatric diseases such as ...
Optimization of pyrrolo[3,4‐f]indole‐5,7‐dione and indole‐5,6‐dicarbonitrile derivatives as inhibitors of monoamine oxidase
(Wiley, 2019)
In recent studies, we have investigated the monoamine oxidase (MAO) inhibition properties of pyrrolo[3,4‐f]indole‐5,7‐dione and indole‐5,6‐dicarbonitrile derivatives. Since numerous high potency MAO inhibitors are present ...