College of Pharmacy, Hainan Medical University, Haikou 571199, China
| Abstract: | Objective To design and synthesize β-lactam triazole compounds. Methods Using triazole and 6-aminopenicillanic acid as starting materials, a series of β-lactam triazole compounds were synthesized based on the principle of active splicing. The molecular structures were characterized by 1H NMR, 13C NMR and mass spectrometry. The antibacterial activity and the ability to inhibit β-lactamase of the target compounds were then determined. Results Three target compounds not reported in the literature were synthesized. After three batches of repeated experiments, the minimum inhibitory concentration of the compounds was determined: the negative control group showed stable bacterial growth, and the blank control group had no bacterial growth, indicating the validity and reliability of the antibacterial ability of the compounds themselves; the inhibitory effect of the compounds on β-lactamase activity was determined: CX-1 (target compound 1) had potential β-lactamase inhibitory properties, while the structurally similar CX-2 (target compound 2) and CX-3 (target compound 3) had relatively weak effects, but all had inhibitory effects on β-lactamase. Conclusion This study holds significant importance for future research directions. By leveraging the findings from this study, researchers can focus on modifying the molecular structures of these β-lactam triazole compounds to discover new compounds with enhanced antibacterial efficacy and more straightforward synthetic routes. |
| Keywords: | Triazole; β-Lactam; Antibiotic; Antibacterial Activity |
| DOI: | 10.57237/j.cse.2025.01.002 |
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