湖南中医药大学学报2017，Vol.37Issue(5)：489-492,4.DOI:10.3969/j.issn.1674-070X.2017.05.007
水杨酰苯胺类mglu5拮抗剂的设计、合成及活性研究
Design, Synthesis, and Activity Screening of New Potent Mglu5 Receptor Antagonists Based on the Salicylanilide Structure
摘要
Abstract
Objective To design, synthesis and activity screening of salicylanilides as new mglu5 receptor antagonist. Methods A scaffold hopping approach has been exploited to design a novel class of mglu5 receptor antagonists I-IV. The design compounds were synthesized by using salicylic acids and anilines. The structures of target compounds were identified by NMR and MS. The activity of mglu 5 was screened by Ca2+ mobilization assay. Results The designed salicylanilides show potent antagonistic activity to mglu5 receptor in vitro. Among them, compound I was the best, and IC50 of compound I was 0.079 μmol/L. Conclusion The salicylanilides were new potent mglu5 receptor antagonist and worth to be further studied.关键词
水杨酰苯胺/代谢型谷氨酸受体5拮抗剂/骨架跃迁Key words
salicylanilide/mglu5 receptor antagonist/scaffold hopping分类
医药卫生引用本文复制引用
傅榕赓,杨辰枝子,严建业,翁臻,周鑫,李林和,熊广华,廖端芳..水杨酰苯胺类mglu5拮抗剂的设计、合成及活性研究[J].湖南中医药大学学报,2017,37(5):489-492,4.基金项目
湖南省自然科学基金项目(2015JJ6085) （2015JJ6085）
湖南省教育厅资助科研项目(13B080) （13B080）
2015药学湖南省重点学科开放基金项目 （）
2015中医药国际合作专项基金资助项目(ZYGZ201502) （ZYGZ201502）
湖南中医药大学本科教学质量工程项目(ZY-005). （ZY-005）
