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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。
Objective To design and synthesize phenolic 2-acetamido-2-deoxy-β-D-glucopyranoside and study its antidepressant activity. Methods The target compounds were synthesized by N-acetylglucosamine as starting material and the structures were confirmed by 1H-NMR, 13C-NMR, IR and high-resolution mass spectrometry. The classical anti-depressant animal model (TST), forced mouse swimming (FST), reserpine antagonism, mouse 5-HTP enhancement experiments on some compounds for antidepressant activity screening. RESULTS AND CONCLUSIONS Twelve compounds were designed and synthesized, of which eight were new compounds not reported in the literature. Five of the compounds were screened for antidepressant activity. Three of them showed significant antidepressant activity and were worth further research and development.