高等学校化学学报

高等学校化学学报 ›› 2005, Vol. 26 ›› Issue (4): 683.

• 研究简报 • 上一篇    下一篇

四甲基吡嗪衍生物合成及其5-HT3受体拮抗活性的筛选

江相清, 黄传满, 祝丽萍, 叶德泳   

  1. 复旦大学药学院, 上海 200032
  • 收稿日期:2004-03-16 出版日期:2005-04-10 发布日期:2005-04-10
  • 通讯作者: 叶德泳(1957年出生),男,教授,从事药物设计与合成研究.E-mail:dyye@shmu.edu.cn E-mail:dyye@shmu.edu.cn

Synthesis of the Derivatives of Tetramethylpyrazine and Screening for 5-HT3 Receptor Antagonistic Activity

JIANG Xiang-Qing, HUANG Chuan-Man, ZHU Li-Ping, YE De-Yong   

  1. School of Pharmacy, Fudan University, Shanghai 200032, China
  • Received:2004-03-16 Online:2005-04-10 Published:2005-04-10

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关键词: 四甲基吡嗪衍生物, 5-HT3受体拮抗剂, 构效关系

Abstract: According to the principle of bioisosterism and the Evans'pharmacophore model of 5-HT3 receptor antagonists, twelve derivatives of tetramethylpyrazine were synthesized. The structures of the compounds were confirmed by MS, 1H NMR and HRMS. All the target compounds are unreported. The preliminary activity test showed that most of the compounds had fairly potent 5-HT3 receptor antagonistic activities, especially compound 3c. And the conformational analysis showed that the active conformation of the compounds was quite fitted to the Evans'pharmacophore model. This indicates that besides the three pharmacophoric elements, the aromatic ring and the substituents attached may affect the bioactivities of the compounds.

Key words: Derivatives of tetramethylpyrazine, 5-HT3 Receptor antagonistic inhibitor, Structure-activity relationship(SAR)

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