Postgraduate Program in Pharmaceutical Sciences-Federal University of Pernambuco, Av. Prof. Moraes Rego, 1235 - University City, Recife, PE, 50740-560, Brazil.
Postgraduate Program in Biological Sciences, Federal University of Pernambuco, Recife, PE, 50740-560, Brazil.
Future Med Chem. 2024;16(18):1839-1852. doi: 10.1080/17568919.2024.2385887. Epub 2024 Sep 5.
This work aimed to synthesize a new pyrimidine with potential application against antimicrobial resistance. was synthesized through condensation reaction between and . The antimicrobial evaluation was carried out using the microdilution method in Mueller-Hinton Agar and predictions using different software. has moderate antibiotic activity and high capacity to efficiently modulate antibiotic resistance in . evaluations demonstrated that 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. demonstrate a good pharmacokinetic profile and toxicological. has great potential to go further in investigating its use against antimicrobial resistance.
这项工作旨在合成一种具有潜在应用价值的新型嘧啶类化合物，以对抗抗微生物药物耐药性。该化合物是通过嘧啶和醛的缩合反应合成的。采用微量稀释法在 Mueller-Hinton 琼脂中进行了抗菌评价，并使用不同的软件进行了抗生素预测。该化合物具有中等的抗生素活性和高效调节能力，能够有效调节 中的抗生素耐药性。评价表明，该化合物可能是青霉素结合蛋白 2a 的别构抑制剂，通过降低最小抑菌浓度 64 倍来调节苯唑西林的作用。药代动力学和毒理学评价表明，该化合物具有良好的特性。该化合物具有很大的潜力，可以进一步研究其在对抗抗微生物药物耐药性方面的应用。
