N4-Phenyl modifications 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

被引:30
作者
Huang, Wenwei
Zheng, Wei
Urban, Daniel J.
Inglese, James
Sidransky, Ellen
Austin, Christopher P.
Thomas, Craig J.
机构
[1] NIH, NIH Chem Genome Ctr, Natl Human Genome Res Inst, Bethesda, MD 20892 USA
[2] NIH, Natl Human Genome Res Inst, Med Genet Branch, Bethesda, MD 20892 USA
关键词
triazine; Gaucher disease; glucocerebrosidase; chemical chaperone;
D O I
10.1016/j.bmcl.2007.08.050
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. Published by Elsevier Ltd.
引用
收藏
页码:5783 / 5789
页数:7
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