Secondary metabolites that have been isolated from bacteria, fungi, plants, or animals are referred to as bioactive chemicals. Bioactive chemicals are helpful in a variety of applications due to their intrinsic qualities, which include antibacterial, anti-inflammatory, and antioxidant effects. A wide range of applications, from fictionalized biomaterials and cosmetics to bioremediation and alternative fuels, have been made possible by the discovery of unique features of these molecules. Nevertheless, obstacles including extraction techniques, formulation stability, regulatory concerns, and consumer acceptability must be overcome in order to fully explore the potential of bioactive chemicals. Advances in characterization and optimization strategies, coupled with non-conventional extraction techniques such as pressurization, enzymes, pulse electric fields, ultrasound, or microwaves, have made extraction more commercially viable, particularly for agrowastes and organic residues. This has contributed to the development of a sustainable circular economy. Bioactive chemicals have encouraging prospects for sustainable development and better human health by overcoming these obstacles. This chapter highlights the necessity for coordinated efforts to realize the full potential of bioactive chemicals by offering insights into the opportunities and constraints connected with their utilization across many sectors.