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新型三唑并[4,3-a]吡嗪衍生物的合成与抗菌活性。

Synthesis and Antibacterial Activity of Novel Triazolo[4,3-]pyrazine Derivatives.

机构信息

Faculty of Chemistry and Environmental Science, Guangdong Ocean University, Zhanjiang 524088, China.

出版信息

Molecules. 2023 Nov 30;28(23):7876. doi: 10.3390/molecules28237876.

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-]pyrazine derivatives were synthesized and their structures were characterized using various techniques, such as melting point, H and 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 and Gram-negative strains. In particular, compound exhibited superior antibacterial activities (MICs: 32 μg/mL against and 16 μg/mL against ), which was comparable to the first-line antibacterial agent ampicillin. In addition, the structure-activity relationship of the triazolo[4,3-]pyrazine derivatives was preliminarily investigated.

摘要

传染病对人类健康构成重大挑战,因此迫切需要开发具有优异抗菌活性的新型抗菌药物。我们合成了一系列新型的三唑并[4,3-a]吡嗪衍生物,并通过熔点、氢核和碳核磁共振波谱、质谱和元素分析等多种技术对其结构进行了表征。我们采用微量稀释法评估了所有合成化合物的体外抗菌活性。在所有测试的化合物中,一些化合物对革兰氏阳性菌和革兰氏阴性菌均表现出中等至良好的抗菌活性。特别是化合物 7e 表现出优异的抗菌活性(MICs:对 为 32 μg/mL,对 为 16 μg/mL),与一线抗菌药物氨苄西林相当。此外,我们还初步研究了三唑并[4,3-a]吡嗪衍生物的构效关系。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d5d9/10708386/f67b3569cd68/molecules-28-07876-g001.jpg

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