2. Academic Validation
  3. Oxazolidinone: A promising scaffold for the development of antibacterial drugs

Oxazolidinone: A promising scaffold for the development of antibacterial drugs

  • Eur J Med Chem. 2023 Mar 15:250:115239. doi: 10.1016/j.ejmech.2023.115239.
Shuo Yuan 1,  Dan-Dan Shen 2,  Yi-Ru Bai 3,  Miao Zhang 3,  Tian Zhou 3,  Chong Sun 3,  Li Zhou 4,  Sai-Qi Wang 5,  Hong-Min Liu 6
Affiliations

Affiliations

  • 1 Children's Hospital Affiliated to Zhengzhou University, Henan Children's Hospital, Zhengzhou Children's Hospital, Zhengzhou, 450018, China; School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Zhengzhou University, Zhengzhou, 450001, China. Electronic address: [email protected].
  • 2 Department of Obstetrics and Gynecology, Zhengzhou Key Laboratory of Endometrial Disease Prevention and Treatment Zhengzhou China, The Third Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China.
  • 3 Children's Hospital Affiliated to Zhengzhou University, Henan Children's Hospital, Zhengzhou Children's Hospital, Zhengzhou, 450018, China; School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Zhengzhou University, Zhengzhou, 450001, China.
  • 4 Children's Hospital Affiliated to Zhengzhou University, Henan Children's Hospital, Zhengzhou Children's Hospital, Zhengzhou, 450018, China.
  • 5 The Affiliated Cancer Hospital of Zhengzhou University & Henan Cancer Hospital, Henan Engineering Research Center of Precision Therapy of Gastrointestinal Cancer, Zhengzhou Key Laboratory of Precision Therapy of Gastrointestinal Cancer, Zhengzhou, 450008, China. Electronic address: [email protected].
  • 6 School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Zhengzhou University, Zhengzhou, 450001, China. Electronic address: [email protected].
PMID: 36893700 DOI: 10.1016/j.ejmech.2023.115239
Abstract

Due to the long-term and widespread use of Antibiotics in clinic, the problem of Bacterial resistance is increasingly serious, and the development of new drugs to treat drug-resistant bacteria has gradually become the mainstream direction of Antibiotic research. The oxazolidinone-containing drugs linezolid, tedizolid phosphate and contezolid have been approved to the market, which are effective against a variety of Gram-positive bacterium infections. Moreover, there are also many Antibiotics containing Oxazolidinone fragment under clinical investigation that show good pharmacokinetic and pharmacodynamic properties with unique mechanism of action against resistant bacteria. In this review, we summarized the oxazolidinone-based Antibiotics already on the market or in clinical trials and the representative bioactive molecules, and mainly focused on their structural optimizations, development strategies and structure-activity relationships in hope of insight into the reasonable design for medical chemists to develop new Oxazolidinone antibiotics with highly potency and fewer side effects.

Keywords

Bacterial resistance; Oxazolidinone antibiotics; Structure-activity relationships.

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