Issue 5, 2009
From the journal:

New Journal of Chemistry

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

Peter Dinér,a   Terese Andersson,a   Jimmy Kjellén,b   Karin Elbing,b   Stefan Hohmannb  and  Morten Grøtli*a  

* Corresponding authors

a Department of Chemistry, University of Gothenburg, Kemivägen 10, 41296 Gothenburg, Sweden
E-mail: grotli@chem.gu.se
Fax: +46 31 7723840
Tel: +46 31 7722905

b Department of Cell and Molecular Biology/Microbiology, University of Gothenburg, Medicinaregatan 9E, 41390 Gothenburg, Sweden

Abstract

A series of 4,5-substituted 1,2,3-triazoles was synthesised viaCu(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 p38α MAP kinase, showing IC50 values in the high nanomolar range.

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

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Article information

DOI
https://doi.org/10.1039/B818909A
Article type
Paper
Submitted
24 Oct 2008
Accepted
31 Oct 2008
First published
16 Dec 2008

New J. Chem., 2009,33, 1010-1016

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

P. Dinér, T. Andersson, J. Kjellén, K. Elbing, S. Hohmann and M. Grøtli, New J. Chem., 2009, 33, 1010 DOI: 10.1039/B818909A

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