Synergistic effect of new pyrimidine derivative with oxacilin against methicillin-resistant <i>Staphylococcus aureus</i>

<b>Aim:</b> This work aimed to synthesize a new pyrimidine <b>PYB01</b> with potential application against antimicrobial resistance.<b>Materials & methods: PYB01</b> was synthesized through condensation reaction between <b>3a</b> and <b>3b</b>. The antimicrobial evaluation was carried out using the microdilution method in Mueller-Hinton Agar and <i>in silico</i> predictions using different software.<b>Results: PYB01</b> has moderate antibiotic activity and high capacity to efficiently modulate antibiotic resistance in <i>Staphylococcus aureus</i>. <i>In silico</i> evaluations demonstrated that <b>PYB01</b> 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. <b>PYB01</b> demonstrate a good pharmacokinetic profile and toxicological.<b>Conclusion: PYB01</b> has great potential to go further in investigating its use against antimicrobial resistance.

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Publication Details

Journal
Future Medicinal Chemistry
Published
2024-09-05
DOI
https://doi.org/10.1080/17568919.2024.2385887
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
0.00

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article

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

Erick Costa, Zenaide Severina do Monte, Gláucia Manoella de Souza Lima, Luciana Scotti et al.
Future Medicinal Chemistry
Synthesis and biological activity
article

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

Erick Costa, Zenaide Severina do Monte, Gláucia Manoella de Souza Lima, Luciana Scotti, Renata Priscila Barros de Menezes, Ricardo Oliveira Silva, Sebastião J. de Melo, Marcus Tullius Scotti, Bruna Kelly de Oliveira Silva, Natália Souza
article en

Abstract

<b>Aim:</b> This work aimed to synthesize a new pyrimidine <b>PYB01</b> with potential application against antimicrobial resistance.<b>Materials & methods: PYB01</b> was synthesized through condensation reaction between <b>3a</b> and <b>3b</b>. The antimicrobial evaluation was carried out using the microdilution method in Mueller-Hinton Agar and <i>in silico</i> predictions using different software.<b>Results: PYB01</b> has moderate antibiotic activity and high capacity to efficiently modulate antibiotic resistance in <i>Staphylococcus aureus</i>. <i>In silico</i> evaluations demonstrated that <b>PYB01</b> 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. <b>PYB01</b> demonstrate a good pharmacokinetic profile and toxicological.<b>Conclusion: PYB01</b> has great potential to go further in investigating its use against antimicrobial resistance.

Future Medicinal ChemistryVol. 16(18)
Universidade Federal da Paraíba (BR), Universidade Federal de Pernambuco (BR)
Conselho Nacional de Desenvolvimento Científico e Tecnológico
Zero hunger
Openalex Percentile: Top 89%
Synthesis and biological activity
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