Benzimidazole and its derivatives are used in organic synthesis and they are used in evaluating new product that possesses different biological activities. This review article covers the most active benzimidazole derivatives that have shown considerable biological actions such as antimicrobial, anti-inflammatory, anticancer, anticonvulsant, antidepressant, antioxidant, radioprotective and anti-leishmanial. This review also discusses the structure-activity relationship of the most potent compounds. It can act as an important tool for medicinal chemists to develop newer compounds possessing benzimidazole moiety that could be better agents in terms of efficacy and safety.