Biologically Active 2-Oxazolidinone Derivatives Beyond Antibacterial Activities

Abstract

2-oxazolidinone is well known as a pharmacophore for antibacterial agents represented by two marketed medicines, Linezolid and Tedizolid. On the other hand, there are growing reports on the various biological activities of 2-oxazolidinones beyond antibacterial activities. Therefore, in this review, we provide an overview of the progress of this untraditional area of 2-oxazolidinones in the past 10 years (2011-2021).

Biocatalytic Construction of Spiro-Oxazolidinones via Halohydrin Dehalogenase-Catalyzed Ring Expansion of Spiro-Epoxides

“…Oxazolidinones are an important class of five-membered heterocyclic compounds with diverse applications in organic synthesis. − Additionally, they hold great importance in the field of medicinal chemistry because of their ability to exhibit a broad spectrum of biological activities. − An excellent example is the antibacterial agent linezolid, which is used to treat infections caused by susceptible Gram-positive bacteria. , In the past decades, spirocyclic scaffolds have gained significant attention and have found widespread applications in the fields of pharmaceutical and natural product. − In particular, spiro-oxazolidinones possess a distinct combination of spirocyclic and oxazolidinone motifs, which confer unique properties to these compounds and open up new avenues for drug design and development. As shown in Scheme , spiro-oxazolidinones have demonstrated a wide range of biological activities, including anticancer, anti-inflammatory, antiviral, antithrombosis, and antidiabetic complications. − Fenspiride, for example, possesses selective β2-adrenergic receptor agonist activity and is used to treat respiratory conditions …”