Synthesis and Evaluation of Chroman-4-One Linked to N-Benzyl Pyridinium Derivatives as New Acetylcholinesterase Inhibitors.
Arch Pharm (Weinheim)
; 348(9): 643-9, 2015 Sep.
Article
em En
| MEDLINE
| ID: mdl-26192069
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 (IC50 = 0.048 µM). 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.
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Base de dados:
MEDLINE
Assunto principal:
Acetilcolinesterase
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Compostos de Piridínio
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Compostos de Benzil
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Inibidores da Colinesterase
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article