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.

含氮杂环是市场上约80％的药物中最常见的结构基序之一。其中，已知苯并咪唑类似物会引起广泛的药物活性，例如抗癌，抗菌，抗寄生虫，抗病毒，抗真菌以及化学感应作用。基于苯并咪唑核心稠合的杂环化合物，开发了新月形的双苯并咪唑类化合物，它们在序列特异性DNA识别方面提供了较早的突破。多年来，双苯并咪唑核心的许多功能变化已导致其独特性质的出现，并将其确立为针对几种病原体的通用配体。