Microorganism-caused diseases are one of the greatest predicaments faced by the world. The disease conditions are worsened due to the development of microbial resistance against numerous antimicrobial agents like quinolones, vancomycin, macrolides, tetracyclines, β-lactam antibiotics, etc. There will always be a vital need to discover new chemotherapeutic agents to avert the emergence of resistance and ideally shorten the duration of therapy. There are various ways to overcome these problems, one of which is to properly utilize the marketed anti-microbials and the other is the synthesis of new antimicrobial compounds. In medicinal chemistry, one of the most potent and biologically active classes to be considered includes the Benzimidazoles. Different benzimidazoles analogues were synthesized by structure modifications. As a result, numerous types of benzimidazole analogues have been synthesized so far and for their chemotherapeutic importance, screened. The aforementioned review summarizes the chemistry of different benzimidazole derivatives formed by substitution at 1st and 2nd position and their applications as antimicrobial agents.