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

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.

Citation

Greco, C., Catania, R., Balacco, D. L., Taresco, V., Musumeci, F., Alexander, C., Huett, A., & Schenone, S. (2020). Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors. Molecules, 25(22), Article 5354. https://doi.org/10.3390/molecules25225354

• Journal Article Type: Article
• Acceptance Date: Nov 9, 2020
• Online Publication Date: Nov 16, 2020
• Publication Date: Nov 16, 2020
• Deposit Date: Nov 17, 2020
• Publicly Available Date: Nov 17, 2020
• Journal: Molecules (Basel, Switzerland)
• Electronic ISSN: 1420-3049
• Publisher: MDPI
• Peer Reviewed: Peer Reviewed
• Volume: 25
• Issue: 22
• Article Number: 5354
• DOI: https://doi.org/10.3390/molecules25225354
• Keywords: Organic Chemistry
• Public URL: https://nottingham-repository.worktribe.com/output/5048891
• Publisher URL: https://www.mdpi.com/1420-3049/25/22/5354