Synthesis of heterocylic compound has always drawn the attention of chemist over the years mainly because of their important biological properties. Particularly, the role of beta-lactam which are endowed with unique structure and potent biological activity. The beta-lactam heterocycles are considered as an important contribution of science to humanity since they have been constituents of living organisms, natural products, drugs and many more substances useful to mankind and society in all walks of life. Their synthesis and evaluation has always drawn the attention of biologists over the years. beta-lactam, a four member heterocyclic compound involved in research aimed to evaluate new products that possess interesting biological activities. Natural and synthetic beta-lactam derivatives occupy a central place among medicinally important compounds due to their diverse and interesting antibiotic activities and are still the most prescribed antibiotics used in medicine. The present review article focuses on the pharmacological profile of beta-lactam with their potential activities. The ring system exhibits a wide range of activities like antimicrobial, antitubercular, anticancer, antidiabetic, tryptase and chymase inhibitory activity etc. attracting the attention of researchers. The biological profile of beta-lactam reported by organic chemist is reviewed here comprehensively with examples under eleven different activities.