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含有2,3-双（苯基氨基）喹喔啉的化合物对耐甲氧西林金黄色葡萄球菌、粪肠球菌及其生物膜具有活性。

Compounds Containing 2,3-Bis(phenylamino) Quinoxaline Exhibit Activity Against Methicillin-Resistant Staphylococcus aureus, Enterococcus faecalis, and Their Biofilms.

作者信息

Padalino Gilda, Duggan Katrina, Mur Luis A J, Maillard Jean-Yves, Brancale Andrea, Hoffmann Karl F

机构信息

Swansea University Medical School, Swansea, UK.

Department of Life Sciences (DLS), Aberystwyth University, Aberystwyth, UK.

出版信息

Microbiologyopen. 2024 Dec;13(6):e011. doi: 10.1002/mbo3.70011.

DOI:10.1002/mbo3.70011
PMID:39665231
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11635387/
Abstract

Antimicrobial resistance remains a global issue, hindering the control of bacterial infections. This study examined the antimicrobial properties of 2,3-N,N-diphenyl quinoxaline derivatives against Gram-positive, Gram-negative, and Mycobacterium species. Two quinoxaline derivatives (compounds 25 and 31) exhibited significant activity against most strains of Staphylococcus aureus, Enterococcus faecium, and Enterococcus faecalis tested, with MIC values ranging from 0.25 to 1 mg/L. These compounds also showed effective antibacterial activity against methicillin-resistant S. aureus (MRSA) and vancomycin-resistant E. faecium/E. faecalis (VRE) strains. They demonstrated comparable or superior activity to four current antibiotics (vancomycin, teicoplanin, daptomycin, and linezolid) against a wide range of clinically relevant isolates. Additionally, they were more effective in preventing S. aureus and E. faecalis biofilm formation compared to several other antibiotics. In summary, these two quinoxaline derivatives have potential as new antibacterial agents.

摘要

抗菌耐药性仍然是一个全球性问题，阻碍了细菌感染的控制。本研究考察了2,3-N,N-二苯基喹喔啉衍生物对革兰氏阳性菌、革兰氏阴性菌和分枝杆菌属菌种的抗菌特性。两种喹喔啉衍生物（化合物25和31）对大多数测试的金黄色葡萄球菌、粪肠球菌和屎肠球菌菌株表现出显著活性，最低抑菌浓度（MIC）值范围为0.25至1毫克/升。这些化合物对耐甲氧西林金黄色葡萄球菌（MRSA）和耐万古霉素粪肠球菌/屎肠球菌（VRE）菌株也显示出有效的抗菌活性。针对多种临床相关分离株，它们表现出与四种现有抗生素（万古霉素、替考拉宁、达托霉素和利奈唑胺）相当或更优的活性。此外，与其他几种抗生素相比，它们在预防金黄色葡萄球菌和粪肠球菌生物膜形成方面更有效。总之，这两种喹喔啉衍生物有潜力成为新型抗菌剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/2d0508764780/MBO3-13-e011-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/d09a26116dc5/MBO3-13-e011-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/cf548614b611/MBO3-13-e011-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/1c246b506a89/MBO3-13-e011-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/b70c19729b24/MBO3-13-e011-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/2d0508764780/MBO3-13-e011-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/d09a26116dc5/MBO3-13-e011-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/cf548614b611/MBO3-13-e011-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/1c246b506a89/MBO3-13-e011-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/b70c19729b24/MBO3-13-e011-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8429/11635387/2d0508764780/MBO3-13-e011-g010.jpg

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本文引用的文献

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Current developments in antibiotic discovery: Global microbial diversity as a source for evolutionary optimized anti-bacterials: Global microbial diversity as a source for evolutionary optimized anti-bacterials.当前抗生素发现的进展：作为进化优化抗菌剂来源的全球微生物多样性：作为进化优化抗菌剂来源的全球微生物多样性。
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