噁唑烷酮类抗菌药研究进展

Progress on Oxazolidinone Antibacterial Agents

在世界范围内,细菌耐药性问题日益严重,已严重影响了感染性疾病的治疗。新型抗耐药菌药物的研究已成为抗菌药物研究的主要方向。噁唑烷酮类化合物是一类新型的治疗细菌性感染的化学全合成药物,具有抑制多重耐药的革兰阳性菌的功效。且作用机制独特,不易与其他药物发生交叉耐药性,从而得到了广泛的研究。在第一个噁唑烷酮类抗菌药物利奈唑胺成功上市后,又有新的化合物进入临床研究,并取得了良好的临床治疗效果。论文介绍了噁唑烷酮类抗菌药的作用机制、抗菌活性、构效关系及最新的噁唑烷酮类抗菌药的研究,为研发新型噁唑烷酮类抗菌药提供参考。

The problem of increasing bacterial resistance has seriously threatened the patients with infectious diseases around the world.As a result,the development of novel antibacterial agents against resistant bacteria has become the main direction of antimicrobial research.Oxazolidinone compounds are a new class of totally-synthetic antibacterial agents for the treatment of bacterial infections and can inhibit multi-drugresistant Gram-positive pathogens.Oxazolidinones possess the unique action of mechanism and low cross resistance to other antibacterials,and therefore have been widely studied.After the first oxazolidinone antibacterial-linezolid launching into international market successfully,new oxazolidinone compounds were introduced into clinical research,and good clinical treatment results were obtained.In this paper,the action mechanism,antibacterial activity,structure-activity relationship of oxazolidinones and the latest studies on oxazolidinone antimicrobials were introduced.It laid the foundation for the development of new oxazolidinone antibacterials.