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.
According to the principle of bioisosterism and the Evans′pharmacophore model of 5-HT_3 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-HT_3 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.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2005年第4期683-685,共3页
Chemical Journal of Chinese Universities
关键词
四甲基吡嗪衍生物
5-HT3受体拮抗剂
构效关系
Derivatives of tetramethylpyrazine
5-HT_3 Receptor antagonistic inhibitor
Structure-activity relationship(SAR)
