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学科主题: 氟化学
题名: Synthesis and biological evaluation of glycosidase inhibitors: gem-difluoromethylenated nojirimycin analogues
其他题名: 糖甘酶抑制剂的合成与生物化学研究:二氟亚甲基Nojirimycin类似物
作者: Wang RW(王若文) ; Qiu XL(邱小龙) ; Mikael Bols ; Fernando Ortega-Caballero ; Qing FL(卿凤翎)
通讯作者: 卿凤翎
刊名: J. Med. Chem.
发表日期: 2006
卷: 49, 期:10, 页:2989-2997
收录类别: SCI
部门归属: 中科院上海有机化学研究所; 东华大学; University of Aarhus
英文摘要: In our ongoing program aimed at the design, synthesis, and biological evaluation of novel gem-difluoromethylenated glycosidase inhibitors, gem-4,4-difluoromethylenated iminosugars (5-9) were synthesized. The biological evaluation of these synthetic iminosugars showed that the gem-difluoromethylenyl group generally reduced the inhibition of glycosidases. However, this was not the case at pH 5.0, where the gem-difluoromethylenated iminosugar 6 was a stronger inhibitor than comparable iminosugars 1 and 36, suggesting that the influence of this group is mainly through its effect on the amine. It is proposed that the unprotonated iminosugar is the species preferably bound by beta-glucosidase, due to the lower pK(a) value of iminosugar 6 than of 1 or 36, leaving iminosugars 1 and 36 mostly protonated at pH 5.0, while iminosugar 6 is not. Iminosugar 6 also displayed good and selective inhibition of beta-glucosidase at pH 6.8.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000237555400014
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/17579
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:
Wang RW,Qiu XL,Mikael Bols,et al. Synthesis and biological evaluation of glycosidase inhibitors: gem-difluoromethylenated nojirimycin analogues[J]. J. Med. Chem.,2006,49(10):2989-2997.
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