It has been demonstrated that most of the various derivatives of benzimidazole have distinct biological activity that gives clear promises to treat many different diseases, and for this wonderful reason, all the different new formulations based on benzimidazole remain of high concentration of interest to most scientists interested in the pharmacological fields. In this review article, we focused on mentioning many different derivatives of benzimidazole and studying its biological activities for humans and animals alike. In addition, in this reference article we have also focused on the more active benzimidazole derivatives that have shown significant pharmacological effect among patients.