Diketopiperazines (DKPs) are small cyclic compounds formed from the condensation of two amino acids. They consist of a six-membered ring containing two carbonyl groups and two nitrogen atoms. DKPs are found in various natural sources, including fungi, bacteria, and plants, and can also be synthesized in laboratories. These compounds have garnered interest in medicinal chemistry due to their diverse biological activities, such as antimicrobial, anticancer, and neuroprotective effects. Research continues to explore their potential applications in drug development and as functional food ingredients, highlighting their significance in both health and industry.