酚性2-乙酰氨基-2-脱氧-β-D-吡喃葡萄糖苷的合成及抗抑郁活性  

Synthesis and anti-depression activities of phenolic 2-acetamido-2-deoxy-β-D-glucopyranoses

作　　者：韩武建 杨蓉 戴晓畅[2] 

机构地区：[1]中美合资昆明贝克诺顿制药有限公司,云南昆明650100 [2]云南大学教育部自然资源药物化学重点实验室,云南昆明650091

出　　处：《中国药物化学杂志》2009年第2期99-105,共7页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计合成酚性2-乙酰氨基-2-脱氧-β-D-吡喃葡萄糖苷并研究其抗抑郁活性。方法以N-乙酰氨基葡萄糖为起始原料经多步反应合成目标化合物,化合物结构经1H-NMR、13C-NMR、IR、高分辨质谱确证;选择经典的抗抑郁动物模型——小鼠悬尾(TST)、强迫小鼠游泳(FST)、利血平拮抗、小鼠5-HTP增强实验等对部分化合物进行抗抑郁活性的筛选。结果与结论设计合成了12个化合物,其中有8个是未见文献报道的新化合物。对合成的5个化合物进行抗抑郁活性筛选,发现有3个表现出明显的抗抑郁活性,有进一步研究开发的价值。Aim To design and synthesize phenolic 2-acetamido-2-deoxy-β-D-glucopyranoses and to investigate their anti-depression activities. Methods According to the structure of 2-acetamido-2-deoxy-β-D-glucopyranoses,twelve target compounds were designed and synthesized. All of them were confirmed by ^1H- NMR, ^13C-NMR respectively, and the new compounds were confirmed by IR and HRMS, then the screening for anti-depression activities of five target compounds were done with TST, FST, reserpine reversal and 5- hydroxytryptophan potentiation in mice. Results Eight compounds are firstly reported, the screening results show that three compounds exhibit obvious anti-depression activities. Conclusion Most of the target compounds show obvious anti-depression activities and this kind of compounds deserve further study.

关 键 词：2-乙酰氨基-2-脱氧-β-D-吡喃葡萄糖苷 合成 抗抑郁活性 

分 类 号：R914[医药卫生—药物化学]