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Synergistic effect of new pyrimidine derivative with oxacilin against methicillin-resistant Staphylococcus aureus .

Bruna Kelly de Oliveira SilvaZenaide Severina do MonteErick Caique Santos CostaRicardo Oliveira SilvaNatália Ferreira SouzaRenata Priscila Barros MenezesMarcus Tullius ScottiLuciana ScottiGláucia Manoella de Souza LimaSebastião José de Melo
Published in: Future medicinal chemistry (2024)
Aim: This work aimed to synthesize a new pyrimidine PYB01 with potential application against antimicrobial resistance. Materials & methods: PYB01 was synthesized through condensation reaction between 3a and 3b . The antimicrobial evaluation was carried out using the microdilution method in Mueller-Hinton Agar and in silico predictions using different software. Results: PYB01 has moderate antibiotic activity and high capacity to efficiently modulate antibiotic resistance in Staphylococcus aureus . In silico evaluations demonstrated that PYB01 is probably an allosteric inhibitor of Protein Binding Penicilin 2a and modulates the action of oxacillin by decreasing the minimum inhibitory concentration by 64-times. PYB01 demonstrate a good pharmacokinetic profile and toxicological. Conclusion: PYB01 has great potential to go further in investigating its use against antimicrobial resistance.
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