(2015) Synthesis and Evaluation of Chroman-4-One Linked to N-Benzyl Pyridinium Derivatives as New Acetylcholinesterase Inhibitors. Archiv der Pharmazie. pp. 643-649.
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Abstract
A novel series of chroman-4-one derivatives containing the N-benzyl pyridinium moiety were designed, synthesized, and evaluated for their acetylcholinesterase (AChE) inhibitory activities. Among the various synthesized compounds, (E)-1-(2,3-dibromobenzyl)-4-((7-ethoxy-4-oxochroman-3-ylidene)methyl)pyridinium bromide (8l) depicted the most potent anti-AChE activity (IC<inf>50</inf>=0.048μM). In addition, the molecular modeling study allowed us to detect possible binding modes that are in full compliance with the observed results through in vitro experiments. A novel series of chroman-4-one derivatives bearing N-benzyl pyridinium derivatives (8a-l) were synthesized and evaluated in vitro for their acetylcholinesterase inhibitory activities. The most promising compound, (E)-1-(2,3-dibromobenzyl)-4-((7-ethoxy-4-oxochroman-3-ylidene)methyl)pyridinium bromide 8l, showed an IC<inf>50</inf> value of 0.048μM. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
| Item Type: | Article |
|---|---|
| Keywords: | 1 (2 bromobenzyl) 4 ((7 ethoxy 4 oxochroman 3 ylidene)methyl)pyridinium bromide; 1 (2 bromobenzyl) 4 ((7 methoxy 4 oxochroman 3 ylidene)methyl)pyridinium bromide; 1 (2,3 dibromobenzyl) 4 ((7 ethoxy 4 oxochroman 3 ylidene)methyl)pyridinium bromide; 1 (2,3 dibromobenzyl) 4 ((7 methoxy 4 oxochroman 3 ylidene)methyl)pyridinium bromide; 1 (4 bromobenzyl) 4 ((7 methoxy 4 oxochroman 3 ylidene)methyl)pyridinium bromide; 1 (4 chlorobenzyl) 4 ((7 ethoxy 4 oxochroman 3 ylidene)methyl)pyridinium bromide; 1 (4 fluorobenzyl) 4 ((7 methoxy 4 oxochroman 3 ylidene)methyl)pyridinium bromide; 1 benzyl 4 ((7 ethoxy 4 oxochroman 3 ylidene)methyl)pyridinium bromide; 1 benzyl 4 ((7 methoxy 4 oxochroman 3 ylidene)methyl)pyridinium bromide; 4 ((7 ethoxy 4 oxochroman 3 ylidene)methyl) 1 (2 fluorobenzyl)pyridinium bromide; 4 ((7 ethoxy 4 oxochroman 3 ylidene)methyl) 1 (4 nitrobenzyl)pyridinium bromide; 4 ((7 methoxy 4 oxochroman 3 ylidene)methyl) 1 (4 methylbenzyl)pyridinium bromide; 4 chromanone derivative; donepezil; n benzyl pyridinium derivative; pyridinium derivative; unclassified drug, Article; drug design; drug screening; drug synthesis; IC50; in vitro study; molecular model; observational study; priority journal |
| Page Range: | pp. 643-649 |
| Journal or Publication Title: | Archiv der Pharmazie |
| Volume: | 348 |
| Number: | 9 |
| Publisher: | Wiley-VCH Verlag |
| Depositing User: | ms soheila Bazm |
| URI: | http://eprints.ssu.ac.ir/id/eprint/9249 |
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