Design, synthesis and bioactivity of aryl piperazine benzob1,4oxazine derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 755-763, 2012.
Artigo
em Chinês
| WPRIM
| ID: wpr-276248
ABSTRACT
Compounds with serotonin reuptake inhibition/5-HT(1A) dual activity were used to build 3D pharmacophore model as a training molecules by Discover Studio. Based on the model, 8 novel aryl piperazine benzo[b][1,4] oxazine derivatives were designed and synthesized, and their structures were confirmed by 1H NMR and HR-MS. Biological evaluation illustrated that compounds VI(1) and VI(7) showed potent functional activities at both 5-HT transporter and 5-HT(1A) receptor, which can be used as lead compounds to guide future research of design and synthesis of potent novel compounds.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Oxazinas
/
Farmacologia
/
Piperazinas
/
Plasmídeos
/
Ligação Proteica
/
Relação Estrutura-Atividade
/
Transfecção
/
Desenho de Fármacos
/
Estrutura Molecular
/
Química
Limite:
Animais
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2012
Tipo de documento:
Artigo
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