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Current Landscape and Future Perspective of Oxazolidinone Scaffolds Containing Antibacterial Drugs

Qianqian Zhao, Liang Xin, Yuzhi Liu, Chengyuan Liang, Jingyi Li, Yanlin Jian, Han Li, Zhenfeng Shi, Hong Liu, Wenqiang Cao

2021Journal of Medicinal Chemistry83 citationsDOI

Abstract

The widespread use of antibiotics has made the problem of bacterial resistance increasingly serious, and the study of new drug-resistant bacteria has become the main direction of antibacterial drug research. Among antibiotics, the fully synthetic oxazolidinone antibacterial drugs linezolid and tedizolid have been successfully marketed and have achieved good clinical treatment effects. Oxazolidinone antibacterial drugs have good pharmacokinetic and pharmacodynamic characteristics and unique antibacterial mechanisms, and resistant bacteria are sensitive to them. This Perspective focuses on reviewing oxazolidinones based on the structural modification of linezolid and new potential oxazolidinone drugs in the past 10 years, mainly describing their structure, antibacterial activity, safety, druggability, and so on, and discusses their structure-activity relationships, providing insight into the reasonable design of safer and more potent oxazolidinone antibacterial drugs.

Topics & Concepts

LinezolidAntibacterial activityDruggabilityPharmacologyAntibioticsChemistryDrugPharmacokineticsBacteriaCombinatorial chemistryMedicineBiochemistryVancomycinBiologyStaphylococcus aureusGeneticsGeneSynthesis and Catalytic ReactionsPhenothiazines and Benzothiazines Synthesis and ActivitiesMicrobial Natural Products and Biosynthesis
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