Insight into the Substrate-Based Synthetic Strategies for Benzimidazoles

Abstract: In medicinal chemistry, the benzimidazole nucleus stands as a cornerstone, boasting remarkable pharmacological activities. Over the past century, the synthesis of benzimidazole and its derivatives, coupled with their diverse reactions, has paved the way for significant advancements in drug discovery and development. The unique potential of benzimidazole has attracted considerable interest from medicinal chemists, leading to the discovery of several clinically approved drugs that incorporate the benzimidazole core. Notably, a large number of patents have been granted for research about benzimidazole, underscoring its importance in pharmaceutical innovation. In recent years, there has been a notable surge in interest surrounding the biological applications of benzimidazole, which has doubled the attention it has garnered from researchers across various domains. This review highlights recent developments in the synthesis and structural modification of benzimidazole derivatives, with a focus on their antimicrobial, anticancer, anti-inflammatory, and antiviral properties. It also outlines the Structure-Activity Relationship (SAR) studies that have guided these developments, while discussing contemporary synthetic methodologies and green chemistry approaches used in their preparation. Furthermore, this manuscript explores potential molecular targets and mechanisms of action associated with benzimidazole-based compounds. By summarizing key trends and findings from the past decade, this work aims to provide researchers with insightful perspectives and future directions for the design and discovery of benzimidazole-based drugs. The study explores potential molecular targets and mechanisms of action associated with benzimidazole-based compounds. By summarizing key trends and findings from the past decade, this work aims to provide researchers with insightful perspectives and future directions for the design and discovery of benzimidazole-based drugs.