Over the last few decades, data on the production of benzimidazole and its derivatives, as well as an assessment of their biological activity, have been reviewed. The synthesis and development of novel compounds are discussed historically, since they are considered a significant heterocyclic moiety with a broad variety of medicinal uses. The synthesis of benzimidazoles and their derivatives continues to be a primary focus for synthetic chemistry communities due to their wide range of activities, which include anti-bacterial, anti-viral, anti-fungal, anti-diabetic, anti-helminthic, anti-convulsant, anti-HIVs, anti-hypertensive, anti-cancer, anti-inflammatory, and anti-oxidant. The goal of this study is to provide up-to-date information on the biological activities and synthesis of various benzimidazole derivatives. Additionally, we have attempted to provide an overview of the chemistry involved in the production of several benzimidazole derivatives for use in medicine. Keywords: Benzimidazole, biological activity, synthesis.