四甲基吡嗪衍生物合成及其5-HT_3受体拮抗活性的筛选
Synthesis of the Derivatives of Tetramethylpyrazine and Screening for 5-HT_3 Receptor Antagonistic Activity作者机构：复旦大学药学院上海200032
出 版 物：《高等学校化学学报》 (Chemical Journal of Chinese Universities)
年 卷 期：2005年第26卷第4期
页 面：683-685页
核心收录：
学科分类：1007[医学-药学(可授医学、理学学位)] 081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 100701[医学-药物化学] 10[医学]
主 题：四甲基吡嗪衍生物 5-HT3受体拮抗剂 构效关系
摘 要：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.
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