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

Authors :
de Oliveira Silva BK
do Monte ZS
Santos Costa EC
Silva RO
Souza NF
Barros Menezes RP
Scotti MT
Scotti L
de Souza Lima GM
de Melo SJ
Source :
Future medicinal chemistry [Future Med Chem] 2024; Vol. 16 (18), pp. 1839-1852. Date of Electronic Publication: 2024 Sep 05.
Publication Year :
2024

Abstract

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.

Details

Language :
English
ISSN :
1756-8927
Volume :
16
Issue :
18
Database :
MEDLINE
Journal :
Future medicinal chemistry
Publication Type :
Academic Journal
Accession number :
39235081
Full Text :
https://doi.org/10.1080/17568919.2024.2385887