Design, synthesis and activity of N-acyl-thiochromenothiazol-2-amine as acetylcholinesterase inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1289-1295, 2014.
Artigo
em Chinês
| WPRIM
| ID: wpr-299137
ABSTRACT
A series of novel N-acyl-thiochromenothiazol-2-amine derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase was investigated. N-Acyl-thiochromenothiazol-2-amines were prepared from thiophenol by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 10a was the best in them. The IC50 of 10a to AChE is 7.92 μmol x L(-1), and the value is better than that of rivastigmine. N-Acyl-thiochromenothiazol-2-amine derivatives showed a certain bioactivity in vitro, which were worth further investigation.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Acetilcolinesterase
/
Relação Estrutura-Atividade
/
Tiazóis
/
Benzopiranos
/
Inibidores da Colinesterase
/
Rivastigmina
/
Aminas
/
Metabolismo
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2014
Tipo de documento:
Artigo
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