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学科主题: 氟化学 ; 生命有机化学
题名: Synthesis and biological evaluation of potent glycosidase inhibitors: 4-deoxy-4,4-difluoroisofagomine and analogues
其他题名: 糖苷酶抑制剂的合成和生物活性研究: 4-去氧-4,4-二氟isofagomine和它的类似物
作者: Li RJ(李瑞杰) ; Mikael Bols ; Cyril Rousseau ; Zhang XG(张新刚) ; Wang RW(王若文) ; Qing FL(卿凤翎)
通讯作者: 卿凤翎
刊名: Tetrahedron
发表日期: 2009
卷: 65, 期:18, 页:3717-3727
收录类别: SCI
部门归属: 上海有机所; 哥本哈根大学
英文摘要: A series of 4,4-difluoroisofagomine analogues were synthesized. These compounds were tested for inhibition of eight glycosidases. The 3R,5R isomer 1 is a new and potent inhibitor against beta-glucosidase from almonds with K-i value of 1.2 mu M. The influence of the gem-difluoromethylene group (CF2) on binding to glycosidases is discussed. It is concluded that only non-essential hydroxyl groups can be replaced by the gem-difluoro group and that in Such a case (beta-glycosidase) the change in inhibition is, interestingly, a result of the change in base strength. (C) 2009 Elsevier Ltd. All rights reserved.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000265264400023
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/17653
Appears in Collections:中科院有机氟化学重点实验室_期刊论文

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Recommended Citation:
Li RJ,Mikael Bols,Cyril Rousseau,et al. Synthesis and biological evaluation of potent glycosidase inhibitors: 4-deoxy-4,4-difluoroisofagomine and analogues[J]. Tetrahedron,2009,65(18):3717-3727.
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