Aspects of Oxazole Derivatives in Medicinal Chemistry: Chemical, Biological and Recent Advances

Abstract

Oxazole derivatives are important heterocyclic scaffolds in medicinal chemistry due to their broad biological activities. These five-membered aromatic rings containing oxygen and nitrogen exhibit antimicrobial, antiviral, anticancer, anti-inflammatory, antifungal, and antitubercular properties. Their favorable electronic features and structural rigidity enable strong and selective interactions with diverse biological targets. Recent advances in synthetic methodologies, particularly the van Leusen protocol using tosylmethylisocyanides (TosMICs), have enabled efficient and regioselective oxazole construction. Additionally, magnetically recoverable catalysts offer sustainable and recyclable approaches with improved yields and reduced environmental impact. These developments have expanded the chemical space of oxazole-based compounds, facilitating the design of drug candidates with enhanced pharmacokinetic and pharmacodynamic profiles. This review summarizes recent synthetic strategies, pharmacological activities, structure–activity relationships, and biosynthetic and mechanistic insights highlighting the significance of oxazole motifs in modern drug discovery.