Medicinal chemistry is a science associated with extraction, analysis and chemical synthesis of newer derivatives which finds applications as medicinal agent in identification and treatment of diseases. In this context, this branch of chemistry is establishing a basis of medicinal molecules in therapeutics. The aim to develop new synthetic compounds to be used as drugs requires combined approach of many disciplines such as chemistry of biomolecules and also of biology at molecular level with medicinal chemistry. The chemists and the biologists are working in collaboration in the search of a lead compound for the new medicines or drug molecules or also in case of an ongoing research on a pre-clinical drug molecule. The various other disciplines working in collaboration includes biology, CADD and X-ray crystallography. This team of collaborators discovered various biologically important compounds, one of them is Benzimidazole. Benzimidazoles and the compounds derived from it represent as an active class of biological literature. Following the discovery of benzimidazole, several structural modifications have been included in the benzimidazoles nucleus to increase its biological activity. In this review we are focusing on various synthetic strategies and biological activities of Benzimidazole nucleus.