Benzimidazole plays an important role in the medicinal chemistry and drug discovery with many
pharmacological activities which have made an indispensable anchor for discovery of novel therapeutic agents.
Substitution of benzimidazole nucleus is an important synthetic strategy in the drug discovery process. Therapeutic
properties of the benzimidazole related drugs have encouraged the medicinal chemists to synthesize novel therapeutic
agents. Therefore, it is required to couple the latest information with the earliest information to understand the current
status of benzimidazole nucleus in drug discovery. In the present review, benzimidazole derivatives with different
pharmacological activities are described on the basis of substitution pattern around the nucleus with an aim to help
medicinal chemists for the development of SAR on benzimidazoles for each activity. This article aims to review the work
reported, chemistry and pharmacological activities of benzimidazole derivatives during past years.
Keywords: Benzimidazoles, early rationality, chemistry, pharmacological activities.
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