Due to the broad-spectrum biological activities, fused heterocyclic compounds are one of the most important systems in medicinal chemistry. Among them, the imidazothiazole which contains a bridgehead nitrogen atom has a vital role because of various applications such as anticancer, antimalarial, antiviral, etc. Designing various imidazothiazole scaffolds has become more important because of their several biological applications. The present review paper discusses the numerous biological applications of imidazothiazole scaffolds in the field of medicine. The review would be useful in future drug design for the development of more promising drug-like scaffolds.