Background: Medicinal uses of natural phenolic acids and its synthetic derivatives have been augmented in recent years. Phenolic acids are chemically defined secondary plant metabolitesand being moieties or leads are much versatile in nature with a widescope of biological activities which seek the attention of researchers across the worldto synthesize different derivatives of phenolic acids and screen them for their various biological properties.These compounds are of meticulous interest due to the properties they possess and their occurrence.Based on the convincing evidences reported in the literature, it is suggested that phenolic acids andtheir derivatives are promising molecules as a drug. Objective: The present review article aims to bring together the information on the biosynthesis, metabolism, and sources of phenolic acids and emphasize on the therapeutic potential of phenolic acid and its synthetic derivatives to comprehensively portray the current scenery for researchers interested in designing drugs for furthering this study. Conclusion: Phenolic acids being moieties or lead are much versatile in nature as they possess a wide range of biological activities like antimicrobial, antioxidant, antiviral, antiulcer, anti-inflammatory, antidiabetic, anticancer and many more which offers researchers to explore more about these or many untapped benefits in medicinal field. The information mentioned in this article will be helpful to the forthcoming researchers working in this area. Phenolic acids have massive potential to be investigated for novel medicinal possibilities and for the development of new chemical moieties to treat different diseases of clinical importance.