1. Synthesis and Antibacterial Activity of Novel Triazolo[4,3- a ]pyrazine Derivatives.
- Author
-
Hu Z, Dong H, Si Z, Zhao Y, and Liang Y
- Subjects
- Humans, Pyrazines pharmacology, Anti-Bacterial Agents chemistry, Escherichia coli, Structure-Activity Relationship, Microbial Sensitivity Tests, Molecular Structure, Anti-Infective Agents, Staphylococcal Infections
- Abstract
Infectious diseases pose a major challenge to human health, and there is an urgent need to develop new antimicrobial agents with excellent antibacterial activity. A series of novel triazolo[4,3- a ]pyrazine derivatives were synthesized and their structures were characterized using various techniques, such as melting point,
1 H and13 C nuclear magnetic resonance spectroscopy, mass spectrometry, and elemental analysis. All the synthesized compounds were evaluated for in vitro antibacterial activity using the microbroth dilution method. Among all the tested compounds, some showed moderate to good antibacterial activities against both Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli strains. In particular, compound 2e exhibited superior antibacterial activities (MICs: 32 μg/mL against Staphylococcus aureus and 16 μg/mL against Escherichia coli ), which was comparable to the first-line antibacterial agent ampicillin. In addition, the structure-activity relationship of the triazolo[4,3- a ]pyrazine derivatives was preliminarily investigated.- Published
- 2023
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