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Synthesis of 3-(1,2,3-triazol-1-yl)- and 3-(1,2,3-triazol-4-yl)-substituted pyrazolo[3,4-d]pyrimidin-4-amines via click chemistry: potential inhibitors of the Plasmodium falciparum PfPK7 protein kinase
Department of Chemistry, University of Gothenburg.
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2009 (English)In: Organic and biomolecular chemistry, ISSN 1477-0520, E-ISSN 1477-0539, Vol. 7, no 17, 3421-3429 p.Article in journal (Refereed) Published
Abstract [en]

Efficient routes to 3-(1,2,3-triazol-1-yl)- and 3-(1,2,3-triazol-4-yl)pyrazolo[3,4-d]pyrimidin-4-amines using a one-pot two-step reaction are presented. The two routes give easy access to two different isomers of 1,4-disubstituted triazoles and the target compounds are obtained from a variety of readily available aromatic and aliphatic halides without isolation of potentially unstable organic azide intermediates. Two compounds show activity towards the PfPK7 kinase (IC(50) 10-20 microM) of P. falciparum, the organism responsible for the most virulent form of malaria, and can be regarded as hits useful for further development into lead compounds.

Place, publisher, year, edition, pages
2009. Vol. 7, no 17, 3421-3429 p.
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Chemical Sciences
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URN: urn:nbn:se:uu:diva-121901DOI: 10.1039/b906482fISI: 000268975300011PubMedID: 19675896OAI: oai:DiVA.org:uu-121901DiVA: diva2:306914
Available from: 2010-03-31 Created: 2010-03-31 Last updated: 2017-12-12Bibliographically approved

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Dinér, Peter

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