Bioactive compounds are compounds produced by plants and algae that have pharmacological or toxicological effects on humans and animals. Algae (micro and macro) are a diverse group of autotrophic organisms and a rich source of different bioactive compounds made up of primary metabolites or chemicals directly involved in the metabolism of the algae, such as lipids, amino acids, carbohydrates, and certain secondary metabolites, including vitamins, sterols, and pigments. Due to their structural diversity and biochemical versatility, these bioactive compounds play a significant role in the medical and pharmaceutical industries. These compounds include carotenoids, phenolic compounds, polysaccharides, proteins, and bioactive peptides. These algal bioactive compounds manifest a wide range of biological activities including antioxidant, antimicrobial, antidiabetic, analgesic, antipyretic, and neuroprotective effects. This chapter emphasizes the importance of the diverse range of algal bioactive compounds and their potential in healthcare including the pharmaceutical industry and therapeutic settings. By exploring the potential of these bioactive compounds, this chapter highlights the contribution of algae and algae-derived compounds to modern-day healthcare and human well-being.