Short cut to 1,2,3-triazole-based p38 MAP kinase inhibitors via [3+2]-cycloaddition chemistry

被引:30
|
作者
Diner, Peter [1 ]
Andersson, Terese [1 ]
Kjellen, Jimmy [2 ]
Elbing, Karin [2 ]
Hohmann, Stefan [2 ]
Grotli, Morten [1 ]
机构
[1] Univ Gothenburg, Dept Chem, S-41296 Gothenburg, Sweden
[2] Gothenburg Univ, Dept Cell & Mol Biol Microbiol, S-41390 Gothenburg, Sweden
关键词
TERMINAL ALKYNES; CYCLOADDITION; DENSITY; AZIDES;
D O I
10.1039/b818909a
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of 4,5-substituted 1,2,3-triazoles was synthesised via Cu(I)-catalysed azide-alkyne 1,3-dipolar [2 + 3]-cycloaddition reactions followed by a Suzuki coupling. The 1,2,3-triazoles were evaluated as inhibitors of the p38 alpha MAP kinase, showing IC50 values in the high nanomolar range.
引用
收藏
页码:1010 / 1016
页数:7
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