Design, synthesis and bioactivity of aryl piperazine benzob1,4oxazine derivatives.
- Author:
Yongyong ZHENG
;
Peng XIE
;
Jin ZHANG
;
Jianqi LI
;
Lin GUO
;
Leiping YU
;
Bin ZHOU
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2012;47(6):755-63
- CountryChina
- Language:Chinese
-
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.
