Thiazolidinone heterocyclic based compounds have been extensively explored for their potent pharmacological activities. Among several existed isomers of thiazolidinone according to position of carbonyl group, the 4-thiazolidinones privileged scaffolds showed significant importance in the modern medicinal chemistry. The current minireview highlights the various involvement of 4-thiazolidinones in different diseases as bioactive candidates. This minireview summarises recent developments in the chemical and biological activities of 4-thiazolidinones, which have proven to be extremely significant in the production of numerous compounds and, consequently, the treatment of numerous diseases. Additionally, the resulted enhancement of activity due to certain molecular hybridization of 4-thiazolidinones with other moieties were illustrated. The 4-thiazolidinones and their derivatives are the most significant and well-researched chemicals. A range of biological actions of this family of chemicals are gathered and addressed in this systematic minireview. This minireview discusses the impact of various substituents on molecules' biological activity. The examples given here can serve as a useful guide for developing novel tiny molecules with high biological activity.