Symmetric bis-benzimidazoles as DNA minor groove-binding agents with anti-tumour and antibacterial activity, and the evolution of the drug ridinilazole for the treatment of Clostridium difficile infections

Anne Baron, Christine Le Sann, John Mann

Research output: Contribution to journalArticlepeer-review

Abstract

We report the synthesis of a range of symmetrical bis-benzimidazoles (BBZ) which possess anticancer and antibacterial activities. One of these BBZs has specific activity against Clostridium difficile and is currently in a phase 3 clinical evaluation as the drug ridinilazole. X-ray and computer modelling studies showed that BBZs typically exhibit high specificity for oligonucleotide sequences that occur in the minor groove of DNA.
Original languageEnglish
Article number116656
JournalBioorganic & Medicinal Chemistry
Volume58
Early online date16 Feb 2022
DOIs
Publication statusPublished - Mar 2022

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