| Summary: | 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-<i>a</i>]pyrazine derivatives were synthesized and their structures were characterized using various techniques, such as melting point, <sup>1</sup>H and <sup>13</sup>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 <i>Staphylococcus aureus</i> and Gram-negative <i>Escherichia coli</i> strains. In particular, compound <b>2e</b> exhibited superior antibacterial activities (MICs: 32 μg/mL against <i>Staphylococcus aureus</i> and 16 μg/mL against <i>Escherichia coli</i>), which was comparable to the first-line antibacterial agent ampicillin. In addition, the structure–activity relationship of the triazolo[4,3-<i>a</i>]pyrazine derivatives was preliminarily investigated.
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