European Journal of Medicinal Chemistry p. 270 - 282 (2017)
Update date:2022-08-03
Topics:
AlNeyadi, Shaikha S.
Salem, Alaa A.
Ghattas, Mohammad A.
Atatreh, Noor
Abdou, Ibrahim M.
A new series of pyrimidine derivatives 5, 9a-d and 12a-d was synthesized by an efficient procedure. The antibacterial activity of the new compounds was studied against four bacterial strains. Compound 5 was found to exhibit the highest potency, with?=?1.0?μg/ml, against both Escherichia coli and Pseudomonas aeruginosa when compared with amoxicillin (MIC?=?1.0–1.5?μg/mL). Transmission electron microscope results confirmed that activities against bacteria occurred via rupturing of the cell wall. Molecular modeling results suggested that compounds 5, 9a-d and 12a-d have the potential to irreversibly bind to the penicillin-binding protein (PBP) Ser62 residue in the active site and were able to overcome amoxicillin resistance in bacteria by inhibiting the β-lactamase enzyme. Docking studies showed that compounds 5, 9a-d and 12a-d inhibit the β-lactamase enzyme through covalent bonding with Ser70. The synergistic effect with amoxicillin was studied. The newly synthesized compounds reported in this study warrant further consideration as prospective antimicrobial agents.
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