Design, synthesis and biological activity evaluation of adenosine analogues / 药学学报
Acta Pharmaceutica Sinica
;
(12): 881-886, 2013.
Artículo
en Chino
| WPRIM
| ID: wpr-259536
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:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Farmacología
/
Relación Estructura-Actividad
/
Estructura Molecular
/
Distribución Aleatoria
/
Adenosina
/
Química
/
Hipnóticos y Sedantes
/
Ratones Endogámicos ICR
/
Actividad Motora
Límite:
Animales
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2013
Tipo del documento:
Artículo
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