Heterocyclic compounds containing nitrogen and sulfur, especially those in the thiazole
family, have generated special interest in terms of their synthetic chemistry, which is attributable to
their ubiquitous existence in pharmacologically dynamic natural products and also as overwhelm-
ingly powerful agrochemicals and pharmaceuticals. The thiazolidin-2,4-dione (TZD) moiety plays
a central role in the biological functioning of several essential molecules. The availability of substi-
tutions at the third and fifth positions of the Thiazolidin-2,4-dione (TZD) scaffold makes it a highly
utilized and versatile moiety that exhibits a wide range of biological activities. TZD analogues exhibit
their hypoglycemic activity by improving insulin resistance through PPAR-γ receptor activation, their
antimicrobial action by inhibiting cytoplasmic Mur ligases, and their antioxidant action by scavenging
reactive oxygen species (ROS). In this manuscript, an effort has been made to review the research
on TZD derivatives as potential antimicrobial, antioxidant, and antihyperglycemic agents from the
period from 2010 to the present date, along with their molecular mechanisms and the information on
patents granted to TZD analogues.