摘要
利奈唑胺是第一个由FDA批准上市的噁唑烷酮类抗菌药,能有效地治疗各类革兰阳性菌感染,适应症包括血液感染、皮肤及软组织感染、社区及医院获得性肺炎等,已逐渐成为临床上常用的抗菌药物之一。除了随后上市的磷酸泰地唑胺(tedizolid phosphate,TR701)和康泰唑胺(contezolid,MRX-I),目前还有多个噁唑烷酮类抗感染候选药物处于临床研究。本文对已上市和处于临床试验的噁唑烷酮抗菌药物做了简要的介绍,并对近期噁唑烷酮类药物的结构优化研究进展进行了总结。
Linezolid is the first oxazolidinone antibacterial drug approved by the FDA,which can effectively treat various gram-positive bacterial infections,including blood infections,skin and soft tissue infections,community and hospital-acquired pneumonia.It has become one of the most commonly used antibiotics in clinical.In addition to the recently launched tedizolid phosphate(TR701)and contezolid(MRX-I),several oxazolidinone anti-infective candidates are currently under clinical research.This review briefly introduces the oxazolidinone antibiotics that have been marketed and are in clinical trials,and recent progress on the structure optimization of oxazolidinone drugs is also summarized.
作者
胡宇华
赵欣彤
李天磊
吴松
张文轩
HU Yu-hua;ZHAO Xin-tong;LI Tian-lei;WU Song;ZHANG Wen-xuan(State Key Laboratory of Bioactive Substance and Function of Natural Medicines,Institute of Materia Medica,Chinese Academy of Medical Sciences&Peking Union Medical College,Beijing 100050,China)
出处
《药学学报》
CAS
CSCD
北大核心
2022年第11期3276-3291,共16页
Acta Pharmaceutica Sinica
基金
中国医学科学院医学与健康科技创新工程(2021-I2M-1-069)。
关键词
抗耐药菌感染
噁唑烷酮类抗菌药
结构优化
构效关系
成药性评价
resistant bacterial infection
oxazolidinone antibiotics
structural optimization
structure-activity relationship
druggability evaluation
