Benzimidazole is the heterocyclic compound which contains a phenyl ring fused to an imidazole ring, Benzimidazole analogs are of crucial importance because of their different clinical applications and biological activity. Benzimidazoles are known as an optimistic class of bioactive heterocyclic compounds possessing a wide variety of biological activities. Benzimidazole derivatives play an important role in medical field with so many pharmacological activities such as antimicrobial, antiviral, anticancer activity, antioxidant, antiparasitic, antiproliferative, antitumor, anti-HIV, anticonvulsant, antiprotozoal, analgesic and anti-inflammatory, antihypertensive, anticancer, androgen receptor antagonist, vasorelaxant etc. This review is summarized to understand the chemistry of various derivatives of substituted benzimidazoles with their pharmacological activities.