Synthesis and Antibacterial Activity of Novel Triazolo[4,3-<i>a</i>]pyrazine Derivatives
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 v...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-11-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/28/23/7876 |
| _version_ | 1797399796142571520 |
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| author | Zhang Hu Hongrui Dong Zhenyu Si Yurong Zhao Yuanwei Liang |
| author_facet | Zhang Hu Hongrui Dong Zhenyu Si Yurong Zhao Yuanwei Liang |
| author_sort | Zhang Hu |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-09T01:46:17Z |
| format | Article |
| id | doaj.art-b70ca7352c1742cca23e9d158aaa0e3e |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T01:46:17Z |
| publishDate | 2023-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-b70ca7352c1742cca23e9d158aaa0e3e2023-12-08T15:22:37ZengMDPI AGMolecules1420-30492023-11-012823787610.3390/molecules28237876Synthesis and Antibacterial Activity of Novel Triazolo[4,3-<i>a</i>]pyrazine DerivativesZhang Hu0Hongrui Dong1Zhenyu Si2Yurong Zhao3Yuanwei Liang4Faculty of Chemistry and Environmental Science, Guangdong Ocean University, Zhanjiang 524088, ChinaFaculty of Chemistry and Environmental Science, Guangdong Ocean University, Zhanjiang 524088, ChinaFaculty of Chemistry and Environmental Science, Guangdong Ocean University, Zhanjiang 524088, ChinaFaculty of Chemistry and Environmental Science, Guangdong Ocean University, Zhanjiang 524088, ChinaFaculty of Chemistry and Environmental Science, Guangdong Ocean University, Zhanjiang 524088, ChinaInfectious 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.https://www.mdpi.com/1420-3049/28/23/7876nitrogen-containing heterocyclestriazole compoundstriazolo[4,3-<i>a</i>]pyrazine derivativesantibacterial activity |
| spellingShingle | Zhang Hu Hongrui Dong Zhenyu Si Yurong Zhao Yuanwei Liang Synthesis and Antibacterial Activity of Novel Triazolo[4,3-<i>a</i>]pyrazine Derivatives Molecules nitrogen-containing heterocycles triazole compounds triazolo[4,3-<i>a</i>]pyrazine derivatives antibacterial activity |
| title | Synthesis and Antibacterial Activity of Novel Triazolo[4,3-<i>a</i>]pyrazine Derivatives |
| title_full | Synthesis and Antibacterial Activity of Novel Triazolo[4,3-<i>a</i>]pyrazine Derivatives |
| title_fullStr | Synthesis and Antibacterial Activity of Novel Triazolo[4,3-<i>a</i>]pyrazine Derivatives |
| title_full_unstemmed | Synthesis and Antibacterial Activity of Novel Triazolo[4,3-<i>a</i>]pyrazine Derivatives |
| title_short | Synthesis and Antibacterial Activity of Novel Triazolo[4,3-<i>a</i>]pyrazine Derivatives |
| title_sort | synthesis and antibacterial activity of novel triazolo 4 3 i a i pyrazine derivatives |
| topic | nitrogen-containing heterocycles triazole compounds triazolo[4,3-<i>a</i>]pyrazine derivatives antibacterial activity |
| url | https://www.mdpi.com/1420-3049/28/23/7876 |
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