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简单而高效的合成3-Aryl-2-oxazolidinone支架,使生物膜的功率增加

Audrey R N Ndukwe^1,2, Sophia Hawas³, Jilong Qin³

¹School of Chemistry and Physics, Faculty of Science, Queensland University of Technology, Brisbane, Queensland 4001, Australia.

Molecular pharmaceutics

|June 8, 2023

概括

新的混合抗生素结合氧化氧化物和氧化物部分的oxazolidinones显示出对抗难以治疗的细菌生物膜的承诺,特别是耐甲基黄金葡萄球菌 (MRSA). 这一策略增强了抗生素对抗耐药生物膜的有效性.

科学领域:

药用化学医学化学
抗微生物耐药性抗微生物耐药性
药物发现药物发现药物发现

背景情况:

细菌生物膜是导致持续性,难以治疗的感染的主要原因,对全球死亡率做出了重大贡献.
减少的抗生素管道需要新的治疗策略来对抗感染,特别是那些涉及生物膜的.
包括linezolid在内的oxazolidinones是抗生素的关键类别,但它们对生物膜的有效性需要改进.

研究的目的:

开发具有增强抗菌膜活性的新型3-aryl-2-oxazolidinone衍生物.
为了研究将linezolid与氧化物部分混合的潜力,以克服耐美西林黄金葡萄球菌 (MRSA) 生物膜中抗生素耐药性的可能性.
为了合成和评估皮佩拉津功能化的氧化和它们的氧化联体,以提高抗生素膜的疗效.

主要方法:

直接合成皮佩拉津尼尔功能化的3 - -2-oxazolidinone衍生物.
用一小部分氧化物对氧化的功能化,以创建混合分子.
对MRSA的浮游生物和生物膜形式进行抗微生物敏感性测试.
对合成化合物的药物相似性和口服生物利用性预测的评估.

主要成果:

与linezolid相比,合成的linezolid-nitroxide合物 (11) 显示出明显更高的针对浮游生物MRSA的最小抑制度,但在根除MRSA生物膜方面具有两倍以上的有效性.
一种piperazinyl oxazolidinone衍生物 (10) 显示出类似于的特性,适合进一步开发.
所有测试的化合物都显示出预测好的口服生物可用性,表明口服药物管理的潜力.

结论:

将抗生素与氧化物等分散剂混合化是一种有希望的策略,可以提高对具有挑战性的MRSA生物膜的有效性.
新型piperazinil oxazolidinone衍生物代表了开发下一代抗菌膜剂的宝贵平台.
这种方法提供了一种可行的方法来延长现有的抗生素的治疗寿命,并对抗生物膜相关的感染.

关键词:

黄金葡萄球菌黄金葡萄球菌抗微生物药物是一种抗菌药物.生物膜是一种生物膜.亚氧化物亚氧化物一个叫Oxazolidinone的人.

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