Molecules (Nov 2020)

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

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

DOI
https://doi.org/10.3390/molecules25225354
Journal volume & issue
Vol. 25, no. 22
p. 5354

Abstract

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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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