Structural Diversity of 1,2,4‐, 1,3,4‐, and 1,2,5‐Oxadiazoles: Synthetic Strategies, Drug–Target Interactions, and Emerging Biological Applications

ABSTRACT Oxadiazole is a heterocyclic molecule with five members that contains both oxygen and nitrogen, and it is part of several marketed drugs used for various purposes, highlighting its significance. Due to its broad applications, chemists continuously seek to synthesize therapeutically active oxadiazole derivatives. These compounds can be prepared using various synthesis methods, with ongoing focus on developing greener and more cost‐effective approaches. Common methods from 2020 to 2025 include cyclization, cyclodehydration, condensation, cross‐dehydrogenative coupling, Mitsunobu–Backmann reaction, catalytic reactions, and the Vilsmeier–Haack reaction. These methods will likely be valuable for researchers working on oxadiazole development. Oxadiazole exhibits a variety of biological activities such as insecticidal, anti‐HIV, fungicidal, antidiabetic, acetylcholinesterase inhibition, antioxidant, antibacterial, anti‐inflammatory, anticonvulsant, and anticancer properties. Studying the various target interactions of oxadiazoles is crucial for modern drug discovery and development because it helps explain how drugs affect biological targets to produce therapeutic effects. Understanding these interactions is essential for designing effective drugs, predicting side effects, and discovering new applications for existing drugs.