Functionalized Benzimidazole Scaffolds: Privileged Heterocycle for Drug Design in Therapeutic Medicine

• Published in: Archiv der Pharmazie (Weinheim) Vol. 349; no. 7; pp. 475 - 506
• Main Authors: Ajani, Olayinka O., Aderohunmu, Damilola V., Ikpo, Chinwe O., Adedapo, Adebusayo E., Olanrewaju, Ifedolapo O.
• Format: Journal Article
• Language: English
• Published: Germany Blackwell Publishing Ltd 01.07.2016; Wiley Subscription Services, Inc
• Subjects: Animals; Antibacterial activity; Benzimidazoles - chemical synthesis; Benzimidazoles - chemistry; Benzimidazoles - pharmacology; Cycloaddition; Cytotoxic activity; Drug Design; Drug Resistance - drug effects; HIV-1; Humans; Molecular Docking Simulation; Molecular Structure; Pharmaceutical industry; Rational drug design; Structure-Activity Relationship; HIV-1; Antibacterial activity; Cycloaddition; Cytotoxic activity; Rational drug design
• ISSN: 0365-6233; 1521-4184
• DOI: 10.1002/ardp.201500464

Benzimidazole derivatives are crucial structural scaffolds found in diverse libraries of biologically active compounds which are therapeutically useful agents in drug discovery and medicinal research. They are structural isosteres of naturally occurring nucleotides, which allows them to interact with the biopolymers of living systems. Hence, there is a need to couple the latest information with the earlier documentations to understand the current status of the benzimidazole nucleus in medicinal chemistry research. This present work unveils the benzimidazole core as a multifunctional nucleus that serves as a resourceful tool of information for synthetic modifications of old existing candidates in order to tackle drug resistance bottlenecks in therapeutic medicine. This manuscript deals with the recent advances in the synthesis of benzimidazole derivatives, the widespread biological activities as well as pharmacokinetic reports. These present them as a toolbox for fighting infectious diseases and also make them excellent candidates for future drug design. Recent advances in the chemistry and pharmacological activities of benzimidazole scaffolds are reported, qualifying them as arsenals for combating infectious diseases and making them resourceful tools and a wheel of fortune in therapeutic medicine for drug design.