Properties of benzimidazole and its derivatives have been studied for over hundred years; special interest of researchers triggered by the fact that 5,6-dimethylbenzimidazole is a component of naturally occurring vitamin B12. Several antihelminthic, antacid and antibacterial drugs are known which have benzimidazole moiety as their essential constituent. Additionally, several bis- and trisbenzimidazole based systems are well-known for their interaction with DNA and interference with several DNA associated processes. This account gives an overview of the benzimidazole based systems and their relevance in medicinal chemistry.
Keywords: Antibacterial, DNA-alkylation, intercalation, major- and minor-groove, transcription factor, polymerase, helicase, topoisomerase
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