Nitrogen-containing heterocycles are one of the most common structural motifs in approximately
80% of the marketed drugs. Of these, benzimidazoles analogues are known to elicit a
wide spectrum of pharmaceutical activities such as anticancer, antibacterial, antiparasitic, antiviral,
antifungal as well as chemosensor effect. Based on the benzimidazole core fused heterocyclic
compounds, crescent-shaped bisbenzimidazoles were developed which provided an early breakthrough
in the sequence-specific DNA recognition. Over the years, a number of functional variations
in the bisbenzimidazole core have led to the emergence of their unique properties and established
them as versatile ligands against several classes of pathogens. The present review provides
an overview of diverse pharmacological activities of the bisbenzimidazole analogues in the past
decade with a brief account of its development through the years.