2‐Aminooxazoles: Synthetic Methodologies and Contributions in Drug Discovery as Anticancer and Antibacterial Agents

ABSTRACT 2‐Aminooxazoles represent a distinctive class of heterocyclic compounds featuring a nucleophilic amino group at the 2‐position of the oxazole ring which enables versatile chemical transformations, rendering these compounds valuable intermediates in the synthesis of a broad range of bioactive molecules. Due to their wide spectrum of biological activities—including antibacterial, antiviral, antifungal, anticancer, anti‐inflammatory, antagonist, antioxidant, antidiabetic and antiallergic effects, 2‐aminooxazoles have garnered significant attention in medicinal chemistry. This review provides a comprehensive overview of the synthetic methodologies reported for the preparation of 2‐aminooxazoles, detailing their substrate scope and plausible reaction mechanisms. So far, traditional and conventional methods are being used for synthesis of 2‐aminooxazoles. Nevertheless, in the past couple of decades, novel methods have been developed with the use of relatively new technologies such as microwave irradiation, ultrasonic irradiation, transition metal catalysis and electrochemistry. Furthermore, the review summarizes recent advances in utilizing 2‐aminooxazoles as privileged scaffolds in the development of anticancer and antibacterial agents, with a focus on their structure–activity relationships (SARs). The review also outlines potential prospects in 2‐aminooxazole‐based drug discovery, aiming to stimulate the rational design of more potent and less toxic therapeutic agents.