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Synthesis of 3-(1,2...
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.
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- Klein, Michael, 1971 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry
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- Dinér, Peter, 1976 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry,Department of Chemistry, University of Gothenburg
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Dorin-Semblat, Dominique (författare)
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Doerig, Christian (författare)
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- Grøtli, Morten, 1966 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry
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(creator_code:org_t)
- Royal Society of Chemistry (RSC), 2009
- 2009
- Engelska.
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Ingår i: Organic & biomolecular chemistry. - : Royal Society of Chemistry (RSC). - 1477-0539 .- 1477-0520. ; 7:17, s. 3421-9
- Relaterad länk:
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https://infoscience....
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https://gup.ub.gu.se...
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https://doi.org/10.1...
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https://urn.kb.se/re...
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Abstract
Ämnesord
Stäng
- 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.
Ämnesord
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
Nyckelord
- Amines
- chemical synthesis
- pharmacology
- Inhibitory Concentration 50
- Mitogen-Activated Protein Kinase Kinases
- antagonists & inhibitors
- Plasmodium falciparum
- enzymology
- Protein Kinase Inhibitors
- chemical synthesis
- Protein Kinases
- drug effects
- Protozoan Proteins
- antagonists & inhibitors
- Pyrimidines
- chemical synthesis
- pharmacology
- Structure-Activity Relationship
- Triazoles
- chemical synthesis
- pharmacology
- Chemistry
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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