Background: Heterocyclic compounds play an essential role in biological sys-tems and occur widely in nature. They are fundamental in the development of pharma-ceuticals aimed at combating microbial infections and other biological activities. Phar-macological evaluations have demonstrated their efficacy against diverse bacterial strains. This study investigates the antimicrobial properties of various benzimidazole hy-brids. The findings highlight the significant influence of substituting nitrogenous scaf-folds with various heteroatoms on the potential development of new antimicrobial agents. Objective: This review article is expected to make a substantial contribution to the ad-vancement of efficacious antibacterial medications. The research's goal is to improve the efficacy of combating bacterial infections by utilizing the potent properties of benzimid-azole-based hybrid scaffolds. In the end, this will aid in reducing the global incidence of this contagious illness. Methods: Several nitrogen-containing heterocyclic compounds display substantial poten-tial as antibacterial agents. These compounds possess fused benzene and imidazole nu-clei. These nuclei could change the number of electrons they have, which in turn affects their physiochemical characteristics. The versatility of drugs arises from their capacity to interact with receptors in various modalities, which is a key factor in drug pharmacolog-ical screening. Benzimidazole-based hybrids have demonstrated a wide range of pharma-cological effects, including antibacterial, anti-HIV, anticancer, antimalarial, antiviral, an-tifungal, antioxidant, anti-inflammatory, and anti-tubercular activities. Results: Pyrazole, imidazole, oxazole, thiazole, indole, and benzimidazole are examples of compounds that include nitrogen species. These nitrogen-containing compounds en-gage in metabolic interactions with other molecules within the cell. Nevertheless, an over-abundance of reactive nitrogen species can cause cytotoxicity, causing harm to vital bio-logical macromolecules. But benzimidazole is traditionally the most effective, with a wide range of important qualities, including antibacterial, anti-HIV, anticancer, antima-larial, antiviral, antifungal, antioxidant, anti-inflammatory, and anti-tubercular activities. Conclusion: This study focuses on the efficacy of novel benzimidazole-based hybrid scaffolds in inhibiting microbial growth or eradicating microorganisms. The study pri-marily focuses on recent studies carried out from 2009 to 2024. The study highlights the effectiveness of different benzimidazole-based hybrids using MIC values. More in-depth studies also show that adding electron-withdrawing groups (EWGs) to the nitrogenous framework might make them more effective. Further research is necessary to design strong, least-toxic benzimidazole-based hybrids that can either kill or inhibit multidrug-resistant (MDR) bacteria.
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