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

Chiara Greco, Rosa Catania, Dario Leonardo Balacco, Vincenzo Taresco, Francesca Musumeci, Cameron Alexander, Alan Huett, Silvia Schenone

2020Molecules22 citationsDOIOpen Access PDF

Abstract

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.

Topics & Concepts

KinaseAntimicrobialEscherichia coliPyrimidineChemistryKanamycinStaphylococcus aureusAmpicillinAntibioticsProtein-Serine-Threonine KinasesBiochemistryProtein kinase ABiologyMicrobiologyBacteriaGeneticsGeneBiochemical and Molecular ResearchQuinazolinone synthesis and applicationsSynthesis and biological activity
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