| Novel 2-aryl-3,4,5-trihydroxypiperidines： Synthesis and glycosidase inhibition |
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| 作者单位： | [1]Beijing National Laboratory for Molecular Science （BNLMS）, CAS Key Laboratory of Molecular Recognition and Function, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China [2]Department of Hospital Pharmacy, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan [3]Chemistry Research Laboratory, Department of Chemistry, University of Oxford, Mansfield Road, Oxford OX1 3TA, UK [4]Summit PLC, 91, Milton Park, Abingdon, Oxon OX14 4RY, UK [5]Phytoquest Limited, IBERS, Plas Gogerddan, Ceredigion, Aberystwyth SY23 3EB, Wales, UK |
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| 基金项目： | Acknowledgments Financial support from National Basic Research Program of China （Nos. 2012CB822101 and 2011CB808603）, and the Natural Science Foundation of China （Nos. 21272240 and 21102149） is gratefully acknowledged. |
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| 摘 要： | Three pairs of novel 2-aryl-3,4,5-trihydroxypiperidines （6-8 and their enantiomers）, the piperidine analogues of the pyrrolidine alkaloids radicamine A and radicamine B, were prepared from six- membered cyclic nitrones through a concise two-step procedure, i.e., Grignard reagent addition and deprotection. These novel polyhydroxylated piperidine iminosugars were assayed against 10 types of enzymes. Only compound 8 exhibited weak inhibition （IC50 1080 μmol/L） against β-galactosidase from rat intestinal lactases.
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| 关 键 词： | 半乳糖苷酶 酶抑制 芳基 合成 格氏试剂 IC50 对映体 类似物 |
| 收稿时间： | 19 May 2013 |
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