A review of the past decade of Azlactones: Synthesis, Reactions, Biomedical and Pharmaceutical applications

Azlactones (2,4-disubstituted oxazol-5-ones) are pivotal building blocks in pharmaceutical design due to their dual electrophilic-nucleophilic reactivity and structural plasticity. Their strained ring system enables diverse ring-opening pathways, facilitating rapid construction of peptidomimetics and bioactive conjugates. Recent studies demonstrate potent antibacterial and antifungal properties such as pyridinyl-functionalized azlactones exhibit efficacy against MRSA (MIC = 0.78 µg/mL), while azlactone-triazole hybrids inhibit Candida auris (MIC = 1.56 µg/mL) and Aspergillus fumigatus via ergosterol synthesis disruption. Additionally, spiro-azlactones show anticancer potential against MCF-7 and A549 cell lines through DNA interaction, tubulin polymerization inhibition, and cell cycle disruption. The spirocyclic structure enhances selectivity, target affinity, and metabolic stability.