: 2,4-Thiazolidinediones are a versatile scaffold with a unique structural feature of hydrogen bonding donor and the hydrogen bonding acceptor region. This review deals with the synthesis of various bio-active 2,4-thiazolidinedione derivatives. It is presented on the basis of the linker variations at 3rd & 5th positions of 2,4-thizolidinediones. Biological evaluations of various derivatives thus prepared and toxicity studies on the respective products as given by various researchers/ Research groups have been described.