Synthesis and Characterization of Dihydropyrimidine-2-One Derived Nanoparticles with Enhanced Anti-Bacterial Activity Against Pathogenic/Resistant Microorganisms
摘要
In this study, the efficacy of dihydropyrimidine (DHPM) derived nanoparticles (NPs) was evaluated against pathogenic/resistant microorganisms. Nanoparticles of ethyl 6-methyl-4-(3-nitrophenyl)-2-oxo-3,4-dihydrodropyrimidine-5-carboxylate (DHPM 1) were synthesized using the emulsification-solvent-evaporation method and were characterized by dynamic light scattering, ζ potential, and scanning electron microscopy techniques. The efficacy of the parental compound DHPM 1 and its NPs was determined against the multidrug-resistant (MDR) bacteria. It was observed that the DHPM 1 compound exhibited stronger bactericidal effects at a concentration of 5 mg/mL in both the agar-well diffusion and broth microdilution (BMD) assays. However, the bactericidal activity of the corresponding nanoparticles (NPs; ~200–260 nm) exhibited markedly higher activity, showing potent antimicrobial effects at substantially lower concentrations (≤ 1.25 mg/mL) against all tested bacterial strains. NPs formation of the DHPM 1 resulted in nearly 3.5-fold reduction in MIC (from ≥ 4.5 mg/mL for the parent compound to ≤ 1.25 mg/mL for the NPs), indicating significantly augmented antibacterial activity compared to the parent compound. This enhanced activity of the dihydropyrimidine-derived nanoparticles relative to their parent compound suggests their potential usefulness in the chemotherapy of pathogenic and drug-resistant microorganisms.