聚胺抗生素开发的最新进展:2010-2023年
Cornelis J Slingerland1, Nathaniel I Martin1
1Biological Chemistry Group, Institute of Biology Leiden, Leiden University, Sylviusweg 72, 2333 BE Leiden, The Netherlands.
ACS infectious diseases
|March 12, 2024
概括
聚米克辛是多抗药性格兰氏阴性感染的关键抗生素. 最近的研究重点是新的多胺类同类物来降低毒性和提高疗效,目前有几个在临床试验中.
科学领域:
- 微生物学 微生物学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- 聚米克辛是有效对抗革兰氏阴性细菌的脂抗生素.
- 它们的临床使用正在增加,原因是多药耐药性感染的增加.
- 聚密素毒性机制仍在被阐明.
研究的目的:
- 审查自2010年以来聚胺类同类的最新进展.
- 更新新变种的结构-活性关系和毒性.
- 讨论合成方法的进展,用于polymyxin类似物开发.
主要方法:
- 关于2010年以来发表的研究的文献综述.
- 分析新型多胺类同类物质的结构-活性关系.
- 对模拟生成的合成和半合成方法的检查.
主要成果:
- 几种新型聚胺类同类物表现出有希望的活性和潜在的降低毒性.
- 目前,有三种新的多胺类同类药物正在临床试验中.
- 总合成和半合成的进步使得各种类比的创建成为可能.
结论:
- 新的多胺类类似物显示出克服老药物的局限性的潜力.
- 目前正在进行的研究旨在减轻与多素相关的毒性.
- 合成和半合成聚米克辛的开发为治疗耐药感染提供了希望.
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