All the heterocyclic compounds are of great interest in Pharmaceutical Chemistry. Out of these heterocyclic compounds the benzfused heterocyclic compound, i.e. benzimidazole is an important pharmacophore and privileged structure in medicinal chemistry. Recently many benzimidazole drugs like antiparasitic, thiabendazole, mebendazole and albendazole, antihistaminic norastemizole and mizolastine, as well as antihypertensive telmisartan etc. have been successfully developed and extensively used in clinic. The wide spectrum of biological activities associated with benzimidazole has been of huge interest and its derivatives have wide variety of biological activities like antihelminthic, antiulcer, diuretic, anticonvulsant, analgesic, antiulcer, antihypertensive, anticoagulant, anticancer, antiinflammatory, antimicrobial, antiviral, antiparasitic and antioxidant. This review is summarized different derivatives of substituted benzimidazoles along with their pharmacological activities. This has attracted increasing interest to investigate the possible applications of benzimidazole derivatives in other medicinal aspects.