Thiazolidinone derivatives have garnered a lot of focus lately because of their various biological functions and possible applications in the field of medicinal chemistry. Thiazolidinone derivatives of synthetic origin have shown significant biological potential in medicinal chemistry, with antimicrobial, antioxidant, and antidiabetic activities. Antimicrobial properties have been demonstrated against various pathogenic microorganisms, such as bacteria, fungi, and protozoa. These derivatives have been extensively investigated for their ability to scavenge free radicals and mitigate oxidative stress-induced cellular damage. Antidiabetic properties have emerged as potential candidates for managing diabetes mellitus, modulating key enzymes involved in glucose metabolism and improving insulin sensitivity. Understanding their structure-activity relationships and mechanisms of action can help in developing new therapeutic agents for treating various diseases. Utilizing these biological activities holds great promise for addressing challenges posed by infectious diseases, oxidative stress-related conditions, and diabetes, potentially pave the way for the development of innovative pharmaceutical interventions in the future. This paper focuses on efforts to synthesized and probe their structure activity relationships and mechanisms for the future study. The diverse biological activities, the potential for structural modification, and the need for new therapeutic agents in various disease areas contribute to the prominence of thiazolidinone derivatives in pharmaceutical and chemical research. Continued research in this field has the potential to yield novel drug candidates and contribute to advancements in the pharmaceutical industry.