Design, synthesis and biological activity evaluation of adenosine analogues / 药学学报
Acta Pharmaceutica Sinica
; (12): 881-886, 2013.
Article
em Zh
| WPRIM
| ID: wpr-259536
Biblioteca responsável:
WPRO
ABSTRACT
N6-(2-Hydroxyethyl) adenosine, HEA (1), an active ingredient isolated from cultured mycelia of cordyceps species which is a famous traditional tonic in China, showed brain protective, sedative hypnotic activity in pharmacological tests. In order to explore novel non-benzodiazepine sedative-hypnotic agents, HEA was treated as the lead compound. Twenty three target compounds were designed and synthesized. Their chemical structures were characterized by 1H NMR, MS and elemental analysis. Pharmacological test in vivo showed that target compounds 8, 4, 13 were more active than HEA on locomotor and gasping activities of mice. Structure-activity relationships showed that the ribose moiety at N-9 position of adenine base was critical for activity.
Texto completo:
1
Base de dados:
WPRIM
Assunto principal:
Farmacologia
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Relação Estrutura-Atividade
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Estrutura Molecular
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Distribuição Aleatória
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Adenosina
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Química
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Hipnóticos e Sedativos
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Camundongos Endogâmicos ICR
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Atividade Motora
Limite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2013
Tipo de documento:
Article