Issue 5, 2023

Oxazolidinones as versatile scaffolds in medicinal chemistry

Abstract

Oxazolidinone is a five-member heterocyclic ring with several biological applications in medicinal chemistry. Among the three possible isomers, 2-oxazolidinone is the most investigated in drug discovery. Linezolid was pioneered as the first approved drug containing an oxazolidinone ring as the pharmacophore group. Numerous analogues have been developed since its arrival on the market in 2000. Some have succeeded in reaching the advanced stages of clinical studies. However, most oxazolidinone derivatives reported in recent decades have not reached the initial stages of drug development, despite their promising pharmacological applications in a variety of therapeutic areas, including antibacterial, antituberculosis, anticancer, anti-inflammatory, neurologic, and metabolic diseases, among other areas. Therefore, this review article aims to compile the efforts of medicinal chemists who have explored this scaffold over the past decades and highlight the potential of the class for medicinal chemistry.

Graphical abstract: Oxazolidinones as versatile scaffolds in medicinal chemistry

Article information

Article type
Review Article
Submitted
23 noy 2022
Accepted
06 fev 2023
First published
08 fev 2023
This article is Open Access
Creative Commons BY-NC license

RSC Med. Chem., 2023,14, 823-847

Oxazolidinones as versatile scaffolds in medicinal chemistry

G. F. S. Fernandes, C. B. Scarim, S. Kim, J. Wu and D. Castagnolo, RSC Med. Chem., 2023, 14, 823 DOI: 10.1039/D2MD00415A

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