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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英文版,2017,37(5):489-492.[Click to copy
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| 水杨酰苯胺类mglu5拮抗剂的设计、合成及活性研究 |
| 傅榕赓,杨辰枝子,严建业,翁臻,周鑫,李林和,熊广华,廖端芳 |
| (湖南中医药大学药学院, 湖南 长沙 410208;湖南中医药大学人文社科学院, 湖南 长沙 410208;国家重点学科国家中医药管理局病理生理实验室, 湖南 长沙 410208) |
| 摘要: |
| 目的 利用骨架跃迁思想设计并合成新型水杨酰苯胺类代谢型谷氨酸受体5（metabotropic glutamate receptor 5， mglu5）拮抗剂。方法 将取代水杨酸与二取代苯胺缩合得目标化合物I-IV，用核磁共振和质谱进行结构确证，荧光测钙流法进行拮抗mglu5活性测定。结果 设计的目标化合物对mglu5具有明显的拮抗活性，其中化合物I拮抗活性最好，IC50为0.079 μmol/L。结论 水杨酰苯胺类化合物为潜在的新型mglu5拮抗剂，值得进一步研究。 |
| 关键词: 水杨酰苯胺 代谢型谷氨酸受体5拮抗剂 骨架跃迁 |
| DOI：10.3969/j.issn.1674-070X.2017.05.007 |
| Received:September 23, 2016 |
| 基金项目:湖南省自然科学基金项目（2015JJ6085）；湖南省教育厅资助科研项目（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）；湖南中医药大学本科教学质量工程项目（ZY-005）。 |
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| Design, Synthesis, and Activity Screening of New Potent Mglu5 Receptor Antagonists Based on the Salicylanilide Structure |
| FU Ronggeng,YANG Chenzhizi,YAN Jianye,WENG Zhen,ZHOU Xin,LI Linhe,XIONG Guanghua,LIAO Duanfang |
| (School of Pharmacy, Hunan University of Chinese Medicine, Changsha, Hunan 410208, China;School of Humanities, Hunan University of Chinese Medicine, Changsha, Hunan 410208, China;Hunan Provincial Key Laboratory of Diagnostics of Traditional Chinese Medicine, Hunan University of Chinese Medicine, Changsha, Hunan 410208, China) |
| 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. |
| Key words: salicylanilide mglu5 receptor antagonist scaffold hopping |
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