Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones.
Acetylcholinesterase
butyrylcholinesterase
chalcone
docking
monoamine oxidase-B
thiophene.
Journal
Central nervous system agents in medicinal chemistry
ISSN: 1875-6166
Titre abrégé: Cent Nerv Syst Agents Med Chem
Pays: United Arab Emirates
ID NLM: 101269163
Informations de publication
Date de publication:
2019
2019
Historique:
received:
18
07
2018
revised:
29
10
2018
accepted:
07
11
2018
pubmed:
20
11
2018
medline:
21
11
2019
entrez:
20
11
2018
Statut:
ppublish
Résumé
Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer's disease (AD). The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated. Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 µM. Among the synthesised molecules, T8 and T6 showed the most potent inhibitory activity against AChE and BChE, respectively. Taken together, the data revealed that T8 could be further optimized to enhance its AChE inhibitory activity.
Sections du résumé
BACKGROUND
BACKGROUND
Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer's disease (AD).
METHODS
METHODS
The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated.
RESULTS
RESULTS
Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 µM. Among the synthesised molecules, T8 and T6 showed the most potent inhibitory activity against AChE and BChE, respectively.
CONCLUSION
CONCLUSIONS
Taken together, the data revealed that T8 could be further optimized to enhance its AChE inhibitory activity.
Identifiants
pubmed: 30451121
pii: CNSAMC-EPUB-94622
doi: 10.2174/1871524918666181119114016
doi:
Substances chimiques
Chalcones
0
Cholinesterase Inhibitors
0
Monoamine Oxidase Inhibitors
0
Monoamine Oxidase
EC 1.4.3.4
Acetylcholinesterase
EC 3.1.1.7
Types de publication
Letter
Langues
eng
Sous-ensembles de citation
IM
Pagination
67-71Informations de copyright
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