Oxadiazole derivatives have emerged as an important class of heterocyclic compounds in medicinal chemistry due to their unique structural features, aromatic stability, and broad spectrum of biological activities. The oxadiazole ring, consisting of two nitrogen atoms and one oxygen atom, serves as a versatile pharmacophore and an effective bioisostere for carbonyl-containing functional groups, thereby enhancing metabolic stability, bioavailability, and target specificity of drug candidates. Over the past few decades, extensive research efforts have focused on the synthesis and pharmacological evaluation of oxadiazole-based compounds, leading to the identification of promising therapeutic agents with antimicrobial, anticancer, anti-inflammatory, antitubercular, antidiabetic, and central nervous system–related activities. Advances in synthetic methodologies, including green and microwave-assisted techniques, have further facilitated the rapid development of structurally diverse oxadiazole derivatives. Structure–activity relationship studies have provided valuable insights into the influence of substituents and isomeric forms on biological efficacy and selectivity. Despite certain challenges related to toxicity and bioavailability, ongoing progress in rational drug design and modern synthetic approaches continues to expand the therapeutic potential of oxadiazole scaffolds. This comprehensive review critically summarizes the chemistry, synthesis, pharmacological activities, and future prospects of oxadiazole derivatives as potential therapeutic agents.
Sohail Ahmed1, Neeku Singh2*, Mohd. Israr Tyagi3 (Fri,) studied this question.