Design, synthesis and bioactivity of aryl piperazine benzob1,4oxazine derivatives.
- Author:
Yong-Yong ZHENG
1
;
Peng XIE
;
Jin ZHANG
;
Jian-Qi LI
;
Lin GUO
;
Lei-Ping YU
;
Bin ZHOU
Author Information
1. Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
- Publication Type:Journal Article
- MeSH:
Animals;
CHO Cells;
Cricetinae;
Cricetulus;
Drug Design;
Genetic Vectors;
Molecular Structure;
Oxazines;
chemical synthesis;
chemistry;
pharmacology;
Piperazines;
chemical synthesis;
chemistry;
pharmacology;
Plasmids;
Protein Binding;
Receptor, Serotonin, 5-HT1A;
genetics;
metabolism;
Serotonin Plasma Membrane Transport Proteins;
genetics;
metabolism;
Serotonin Uptake Inhibitors;
metabolism;
Structure-Activity Relationship;
Transfection
- From:
Acta Pharmaceutica Sinica
2012;47(6):755-763
- 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.
