Oxadiazole is an organic compound featuring a heterocyclic ring housing carbon, oxygen,
and nitrogen atoms. Due to their heightened stability in biological environments, oxadiazole rings
exhibit significant biological activities, effectively addressing health challenges like infectious diseases
and chronic conditions in medicinal chemistry. The main objective of this review is to discuss
various synthetic approaches related to oxadiazole and its derivatives, along with their biological
activities. The diverse reactivity positions oxadiazole as a valuable building block in organic synthesis,
with derivatives exhibiting promising pharmacological activities. It involves a systematic literature
review, critical analysis, and synthesis of existing research. This review comprises the everexpanding
chemical knowledge but also holds significant implications for drug development. The
various synthetic approaches, such as Suzuki-Miyaura, Stille coupling [3+2] cycloaddition reaction,
and many more methods used for the synthesis of oxadiazole through different schemes, have been
discussed thoroughly. This review also concisely associated the pharmacological activities of new
oxadiazole and its derivatives, such as prenoxdiazine, dapagliflozin, nesapidil, pleconaril, and so on.
This review highlights the importance of continued research into the structure-activity relationships
of oxadiazole derivatives, paving the way for developing novel and more potent therapeutic agents.