Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
Bioorg Med Chem. 2019 Sep 1;27(17):3760-3774. doi: 10.1016/j.bmc.2019.07.023. Epub 2019 Jul 12.
Multi-drug resistant Staphylococcus aureus infections have created a critical need for the development of new classes of antibacterials. Discovery of new naturally derived antibacterial agents with new mechanism of action remains a high priority globally. Several of the available antibacterial agents like β-lactams, polyketides, phenylpropanoids, aminoglycosides, macrolides, glycopeptides, streptogramins and lipopeptides are natural products or their semisynthetic variations. In the current scenario of alarming rise in antibacterial resistance, revisiting natural products with modern chemistry and biology tools has fascinated many medicinal chemists for discovery and development of natural products or derived semisynthetic derivatives as effective antibacterial agents. This review underlines the structures and anti-MRSA activity of various natural product derivatives covering recent reports, in vivo activities and brief Structure Activity Relationships (SARs).
耐多药金黄色葡萄球菌感染的出现，对新型抗菌药物的研发提出了迫切需求。因此，全球都在高度重视发现具有全新作用机制的新型天然来源抗菌药物。目前有一些抗菌药物，如β-内酰胺类、聚酮类、苯丙素类、氨基糖苷类、大环内酯类、糖肽类、链阳性菌素类和脂肽类，都是天然产物或其半合成变体。在当前抗菌药物耐药性急剧上升的情况下，利用现代化学和生物学工具重新研究天然产物，激发了许多药物化学家的兴趣，他们致力于发现和开发天然产物或衍生的半合成衍生物，以作为有效的抗菌药物。本综述强调了各种天然产物衍生物的结构和抗耐甲氧西林金黄色葡萄球菌（MRSA）活性，涵盖了近期报道的、具有体内活性和简要结构活性关系（SAR）的衍生物。
