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Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors

Pyrazolo[3,4-d]pyrimidines represent an important class of heterocyclic compounds well-known for their anticancer activity exerted by the inhibition of eukaryotic protein kinases. Recently, pyrazolo[3,4-d]pyrimidines have become increasingly attractive for their potential antimicrobial properties. H...

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Autores principales: Greco, Chiara, Catania, Rosa, Balacco, Dario Leonardo, Taresco, Vincenzo, Musumeci, Francesca, Alexander, Cameron, Huett, Alan, Schenone, Silvia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7696985/
https://www.ncbi.nlm.nih.gov/pubmed/33207806
http://dx.doi.org/10.3390/molecules25225354
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author Greco, Chiara
Catania, Rosa
Balacco, Dario Leonardo
Taresco, Vincenzo
Musumeci, Francesca
Alexander, Cameron
Huett, Alan
Schenone, Silvia
author_facet Greco, Chiara
Catania, Rosa
Balacco, Dario Leonardo
Taresco, Vincenzo
Musumeci, Francesca
Alexander, Cameron
Huett, Alan
Schenone, Silvia
author_sort Greco, Chiara
collection PubMed
description Pyrazolo[3,4-d]pyrimidines represent an important class of heterocyclic compounds well-known for their anticancer activity exerted by the inhibition of eukaryotic protein kinases. Recently, pyrazolo[3,4-d]pyrimidines have become increasingly attractive for their potential antimicrobial properties. Here, we explored the activity of a library of in-house pyrazolo[3,4-d]pyrimidines, targeting human protein kinases, against Staphylococcus aureus and Escherichia coli and their interaction with ampicillin and kanamycin, representing important classes of clinically used antibiotics. Our results represent a first step towards the potential application of dual active pyrazolo[3,4-d]pyrimidine kinase inhibitors in the prevention and treatment of bacterial infections in cancer patients.
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spelling pubmed-76969852020-11-29 Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors Greco, Chiara Catania, Rosa Balacco, Dario Leonardo Taresco, Vincenzo Musumeci, Francesca Alexander, Cameron Huett, Alan Schenone, Silvia Molecules Article Pyrazolo[3,4-d]pyrimidines represent an important class of heterocyclic compounds well-known for their anticancer activity exerted by the inhibition of eukaryotic protein kinases. Recently, pyrazolo[3,4-d]pyrimidines have become increasingly attractive for their potential antimicrobial properties. Here, we explored the activity of a library of in-house pyrazolo[3,4-d]pyrimidines, targeting human protein kinases, against Staphylococcus aureus and Escherichia coli and their interaction with ampicillin and kanamycin, representing important classes of clinically used antibiotics. Our results represent a first step towards the potential application of dual active pyrazolo[3,4-d]pyrimidine kinase inhibitors in the prevention and treatment of bacterial infections in cancer patients. MDPI 2020-11-16 /pmc/articles/PMC7696985/ /pubmed/33207806 http://dx.doi.org/10.3390/molecules25225354 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Greco, Chiara
Catania, Rosa
Balacco, Dario Leonardo
Taresco, Vincenzo
Musumeci, Francesca
Alexander, Cameron
Huett, Alan
Schenone, Silvia
Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors
title Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors
title_full Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors
title_fullStr Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors
title_full_unstemmed Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors
title_short Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors
title_sort synthesis and antibacterial evaluation of new pyrazolo[3,4-d]pyrimidines kinase inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7696985/
https://www.ncbi.nlm.nih.gov/pubmed/33207806
http://dx.doi.org/10.3390/molecules25225354
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