Thiophene a five member heterocycles had been found with enormous biological activities with the suitable modifications in the structure. The present review is an attempt made to direct the attention of the researchers towards the thiopene ring for the development of newer chemical entities which are quite useful in the treatment of various life threatening diseases and disorders This review article covers the most active thiopene derivatives that have shown considerable biological actions such as antimicrobial, anti-inflammatory. This review also discusses the structure-activity relationship of the most potent compounds. It can act as an important tool for medicinal chemists to develop newer compounds possessing thiopene moiety that could be better agents in terms of efficacy and safety