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Life sciences · Journal article
Mini-reviews in Medicinal Chemistry · September 25, 2026
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INTRODUCTION: The urgent need for novel antimicrobials to combat antibiotic resistance highlights benzimidazole derivatives as highly promising candidates. Over the past decade, extensive research has focused on the therapeutic potential of benzimidazole-based scaffolds in various pathological conditions, including bacterial infections. METHODS: This review compiles and analyses studies published between 2014 and 2025, highlighting the long history of these molecules in the treatment of various infectious diseases. It also deciphers the latest updates on marketed formulations of benzimidazole derivatives used in infections. Additionally, clinical trials evaluating their efficacy and safety are discussed. Data were extracted regarding synthetic strategies, biological activities, physicochemical properties, and clinical trials. RESULTS: Numerous benzimidazole-based compounds have shown promising results in several in vitro and in vivo investigations. Furthermore, their distinct structural diversity allows for their optimization as antibacterial agents, making them attractive candidates for the development of targeted therapies against specific bacterial pathogens. DISCUSSION: Benzimidazole presents a privileged scaffold suitable for chemical optimization and provides space for structure-guided drug design exploration. These compounds exhibit antibacterial potential via various possible mechanisms, including DNA topoisomerase inhibition, disruption of protein synthesis, and membrane integrity. CONCLUSION: Benzimidazoles and their derivatives demonstrate strong preclinical promise; however, continued structural modification and biological evaluation may advance and translate them into new drug interventions for clinical practice.