文献类型：期刊文献

英文题名：Synthesis and Antibacterial Activity of Novel Triazolo[4,3-a]pyrazine Derivatives

作者：Hu, Zhang[1];Dong, Hongrui[1];Si, Zhenyu[1];Zhao, Yurong[1];Liang, Yuanwei[1];Sabatier, Jean-Marc;Geronikaki, Athina

机构：[1]Guangdong Ocean Univ, Fac Chem & Environm Sci, Zhanjiang 524088, Peoples R China

年份：2023

卷号：28

期号：23

外文期刊名：MOLECULES

收录：SCI-EXPANDED(收录号：WOS:001117583900001)、、Scopus(收录号：2-s2.0-85178946614)、WOS

基金：No Statement Available

语种：英文

外文关键词：nitrogen-containing heterocycles; triazole compounds; triazolo[4,3-a]pyrazine derivatives; antibacterial activity

外文摘要：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, H-1 and C-13 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 mu g/mL against Staphylococcus aureus and 16 mu g/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.