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N2-(2-羟乙基)-6-(吡咯烷-1-基)-1,3,5-三嗪-2,4-二胺的N4-苯基修饰增强了小分子对葡糖脑苷脂酶的抑制作用,这些小分子具有作为戈谢病化学伴侣的潜力。

N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.

作者信息

Huang Wenwei, Zheng Wei, Urban Daniel J, Inglese James, Sidransky Ellen, Austin Christopher P, Thomas Craig J

机构信息

NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892-3370, USA.

出版信息

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5783-9. doi: 10.1016/j.bmcl.2007.08.050. Epub 2007 Aug 28.

Abstract

A series of 1,3,5-triazine-2,4,6-triamines were prepared and analyzed as inhibitors of glucocerebrosidase. Synthesis, structure activity relationships and the selectivity of chosen analogues against related sugar hydrolases enzymes are described.

摘要

制备了一系列1,3,5-三嗪-2,4,6-三胺,并将其作为葡萄糖脑苷脂酶抑制剂进行分析。描述了所选类似物的合成、构效关系及其对相关糖水解酶的选择性。

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