Design, synthesis and antalgic activities of aralkyl-ketone-4-piperidol derivatives / 药学学报
Acta Pharmaceutica Sinica
; (12): 371-378, 2009.
Article
em Zh
| WPRIM
| ID: wpr-278254
Biblioteca responsável:
WPRO
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:
1
Índice:
WPRIM
Assunto principal:
Farmacologia
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Piperidonas
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Relação Estrutura-Atividade
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Medição da Dor
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Estrutura Molecular
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Química
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Limiar da Dor
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Receptores Opioides delta
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Receptores Opioides kappa
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Receptores Opioides mu
Limite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2009
Tipo de documento:
Article