Design, synthesis and antalgic activities of aralkyl-ketone-4-piperidol derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 371-378, 2009.
Artículo
en Chino
| WPRIM
| ID: wpr-278254
ABSTRACT
A series of aralkyl-ketone-4-piperidol derivatives were synthesized and tested for their analgesic activities. All of the novel 30 compounds were prepared from 4-piperidone and alpha-halo-aralkyl-ketone through five steps, including Boc protection, nucleophilic addition in presence of CeCl3/NaI catalyst, deprotection, condensation and salification. Their structures were confirmed by 1H NMR and HRMS. Preliminary in vivo pharmacological trials showed that most of the synthesized compounds revealed analgesic effects. Among the tested compounds, 8, 13 and 22 exhibited potent analgesic activities in both mice writhing and mice hot plate model. The three compounds have low affinity for mu, delta, kappa receptors, which is a chance to find a better precursor of non-opioid analgesic for further optimization.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Farmacología
/
Piperidonas
/
Relación Estructura-Actividad
/
Dimensión del Dolor
/
Estructura Molecular
/
Química
/
Umbral del Dolor
/
Receptores Opioides delta
/
Receptores Opioides kappa
/
Receptores Opioides mu
Límite:
Animales
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2009
Tipo del documento:
Artículo
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