Browsing Faculty of Health Sciences by Subject "Chalcone"
Now showing items 1-10 of 11
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2-Heteroarylidene-1-indanone derivatives as inhibitors of monoamine oxidase
(Elsevier, 2016)In the present study a series of fifteen 2-heteroarylidene-1-indanone derivatives were synthesised and evaluated as inhibitors of recombinant human monoamine oxidase (MAO) A and B. These compounds are structurally related ... -
C3 amino-substituted chalcone derivative with selective adenosine rA1 receptor affinity in the micromolar range
(Springer, 2020)To identify novel adenosine receptor (AR) ligands based on the chalcone scaffold, herein the synthesis, characterization and in vitro and in silico evaluation of 33 chalcones (15–36 and 37–41) and structurally related ... -
Monoamine oxidase inhibitory activities of heterocyclic chalcones
(Elsevier, 2015)Studies have shown that natural and synthetic chalcones (1,3-diphenyl-2-propen-1-ones) possess monoamine oxidase (MAO) inhibition activities. Of particular importance to the present study is a report that a series of ... -
Nitrocatechol derivatives of chalcone as inhibitors of monoamine oxidase and Catechol-O-Methyltransferase
(Bentham Science, 2018)Introduction: The efficacy of L-dopa in the treatment of Parkinson’s disease depends on its metabolic conversion to dopamine in the brain, however extensive peripheral metabolism of L-dopa diminishes its availability for ... -
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. ... -
Selected furanochalcones as inhibitors of monoamine oxidase
(Elsevier, 2013)The validity of the chalcone scaffold for the design of inhibitors of monoamine oxidase has previously been illustrated. In a systematic attempt to investigate the effect of heterocyclic substitution on the monoamine ... -
Structural exploration of synthetic chromones as selective MAO-B inhibitors: a mini review
(Bentham Science, 2017)Aim and Objective: Specific inhibitors of monoamine oxidase (MAO)-B are considered useful therapeutic agents in targeting neurological disorders like Alzheimer's and Parkinson's diseases. Due to the academic challenge of ... -
Synthesis and evaluation of 2-benzylidene-1-tetralone derivatives for monoamine oxidase inhibitory activity
(Bentham Science, 2018)Background: Chalcone has been identified as a promising lead for the design of Monoamine Oxidase (MAO) inhibitors. This study attempted to discover potent and selective chalcone-derived MAO inhibitors by synthesising a ... -
Synthesis and evaluation of C3 substituted chalcone-based derivatives of 7-azaindole as protein kinase inhibitors
(Wiley, 2020)Chalcones are a group of naturally occurring or synthetic compounds which possess a wide range of biological activities. In this paper, a series of twenty‐three 7‐azaindole‐chalcone hybrids (5a–w) were synthesized and ... -
Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters
(Elsevier, 2015)A series of dihydroartemisinyl-chalcone esters were synthesized through esterification of chalcones with dihydroartemisinin (DHA). The hybrids were screened against chloroquine (CQ) sensitive (3D7) and CQ resistant (W2) ...