Privileged structures can bind to multiple targets with high affinity, thus aiding the discovery of novel bioactive agents. Heterocycle- thioacetic acid derivatives, a group of molecules containing a heterocycle core linked with a thioacetic acid-derived fragment, represent an important type of "privileged scaffold" possessing a wide spectrum of biological properties. Numerous encouraging investigations demonstrated that this privileged structure should be extensively exploited for the therapeutic benefits. In view of its predominance, and on the basis of our research interest involved in this scaffold, an updated and detailed account of the pharmacological properties of heterocycle-thioacetic acid derivatives is described in this article.