Background: Selenium (Se) derivatives consistently emerge as vital players in numerous biological functions. These derivatives exhibit potential in addressing various ailments, including cancer, pain, inflammation, neurodegenerative disorders, and infectious diseases. Organo-selenium compounds, given their chemical accessibility and notable pharmacological attributes, represent a burgeoning research area in organoelement chemistry. Purpose: This review aims to shed light on ebselen and its derivatives, emphasizing their potential as bioactive agents. Further, we endeavor to streamline the available literature to provide a clearer understanding of the depth and breadth of research surrounding this topic. Materials and Methods: In aligning with the PRISMA-ScR guidelines, our scoping review strategy entailed a thorough search and curation of studies from the Scopus database. Results: Of the 52 studies initially sourced from Scopus, a total of 10 met the criteria for inclusion in this review. A deep dive into these selected works reveals that organoselenium heterocycles serve as a medium to explore and elucidate selenium compound chemistry. Their benefits span a spectrum - from combating diseases like cancer and Alzheimer's to showcasing antibacterial, antifungal, and antiviral potentials. Conclusion: Drawing from the amassed literature, this review paves the way for understanding future research trajectories. Certain findings underscore their pivotal nature for the conceptualization of optimal compounds. Readers will gain insights into the primary uses of Ebselen and its derivatives as bioactive agents.