Short cut to 1,2,3-triazole-based p38 MAP kinase inhibitors via [3+2]-cycloaddition chemistry
Short cut to 1,2,3-triazole-based p38 MAP kinase inhibitors via [3+2]-cycloaddition chemistry
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DOI：
10.1039/b818909a
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发表时间：
2009-01-01
影响因子：
3.3
通讯作者：
Grotli, Morten
中科院分区：
文献类型：
--
作者：
Diner, Peter;Andersson, Terese;Grotli, Morten
以铜(I)为催化剂，通过叠氮-炔-1，3-偶极[2+3]-环加成反应和Suzuki偶联反应合成了一系列4，5-取代的1，2，3-三氮唑。1，2，3-三氮唑被评价为p38α蛋白激酶的抑制剂，显示IC50值在高纳摩尔范围内。
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.