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

来源：

NEW JOURNAL OF CHEMISTRY | 2009年 / 33卷 / 05期

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

页码：1010 / 1016

页数：7

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