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

doi:10.1016/j.bmc.2022.116656

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^*

^*Corresponding author for this work

School of Chemistry and Chemical Engineering

Research output: Contribution to journal › Review article › peer-review

13 Citations (Scopus)

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 language	English
Article number	116656
Number of pages	3
Journal	Bioorganic & Medicinal Chemistry
Volume	58
Early online date	16 Feb 2022
DOIs	https://doi.org/10.1016/j.bmc.2022.116656
Publication status	Published - 15 Mar 2022

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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. ",

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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. / Baron, Anne; Sann, Christine Le; Mann, John.
In: Bioorganic & Medicinal Chemistry, Vol. 58, 116656, 15.03.2022.

Research output: Contribution to journal › Review article › peer-review

TY - JOUR

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AU - Mann, John

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AB - 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.

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DO - 10.1016/j.bmc.2022.116656

M3 - Review article

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JO - Bioorganic & Medicinal Chemistry

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