(2013) Synthesis of some new 3-coumaranone and coumarin derivatives as dual inhibitors of acetyl- and butyrylcholinesterase. Archiv der Pharmazie. pp. 577-587.
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Abstract
A novel series of coumarin and 3-coumaranone derivatives encompassing the phenacyl pyridinium moiety were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity using Ellman's method. All compounds presented inhibitory activity against both AChE and BuChE in the micromolar range. The molecular docking simulations revealed that all compounds were dual binding site inhibitors of AChE. A kinetic study was performed and the mechanism of enzyme inhibition was proved to be of mixed type. All compounds were tested for their antioxidant activity and no significant activity was observed. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
| Item Type: | Article |
|---|---|
| Keywords: | 1 2 (3,4 dihydroxyphenyl) 2 oxoethyl 4 (6 ethoxy 3 oxobenzofuran 2(3h) ylidene)methylpyridinium chloride; 1 2 (4 bromophenyl) 2 oxoethyl 4 (6 ethoxy 3 oxobenzofuran 2(3h) ylidene)methylpyridinium bromide; 1 2 (4 bromophenyl) 2 oxoethyl 4 3 (8 methoxy 2 oxo 2h chromen 3 yl) 3 oxoprop 1 enylpyridinium bromide; 1 2 (4 fluorophenyl) 2 oxoethyl 4 3 (8 methoxy 2 oxo 2h chromen 3 yl) 3 oxoprop 1 enylpyridinium bromide; 3 coumaranone; 4 (6 ethoxy 3 oxobenzofuran 2(3h) ylidene)methyl 1 (2 oxo 2 p tolylethyl)pyridinium chloride; 4 (6 ethoxy 3 oxobenzofuran 2(3H) ylidene)methyl 1 (2 oxo 2 phenylethyl)pyridinium chloride; 4 (6 ethoxy 3 oxobenzofuran 2(3h) ylidene)methyl 1 2 (4 fluorophenyl) 2 oxoethylpyridinium chloride; 4 3 (8 methoxy 2 oxo 2h chromen 3 yl) 3 oxoprop 1 enyl 1 (2 oxo 2 p tolylethyl)pyridinium bromide; 4 3 (8 methoxy 2 oxo 2h chromen 3 yl) 3 oxoprop 1 enyl 1 (2 oxo 2 phenylethyl)pyridinium chloride; 4 3 (8 methoxy 2 oxo 2h chromen 3 yl) 3 oxoprop 1 enyl 1 2 (4 methoxyphenyl) 2 oxoethylpyridinium bromide; 5,5' dithiobis(2 nitrobenzoic acid); acetylcholinesterase; ascorbic acid; cholinesterase; cholinesterase inhibitor; coumarin derivative; donepezil; pyridinium derivative; unclassified drug, aldol reaction; alkylation; antioxidant activity; article; blood brain barrier; carbon nuclear magnetic resonance; central nervous system; cholinesterase inhibition; cyclization; drug binding site; drug synthesis; hydrogen bond; intestine absorption; microwave irradiation; molecular docking; molecular model; oxidative stress; priority journal; proton nuclear magnetic resonance; structure activity relation, 3-Coumaranone; Actylcholinesterase; Butyrylcholinesterase; Coumarin; Docking study; Phenacyl pyridinium, Acetylcholinesterase; Antioxidants; Butyrylcholinesterase; Cholinesterase Inhibitors; Coumarins; Drug Design; Kinetics; Molecular Docking Simulation; Molecular Structure; Protein Conformation; Structure-Activity Relationship |
| Page Range: | pp. 577-587 |
| Journal or Publication Title: | Archiv der Pharmazie |
| Volume: | 346 |
| Number: | 8 |
| Depositing User: | ms soheila Bazm |
| URI: | http://eprints.ssu.ac.ir/id/eprint/8602 |
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