Article ; Online: 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.
Bioorganic & medicinal chemistry
2022 Volume 58, Page(s) 116656
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 ... ...
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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MeSH term(s) | Anti-Bacterial Agents/chemical synthesis ; Anti-Bacterial Agents/chemistry ; Anti-Bacterial Agents/pharmacology ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Benzimidazoles/chemical synthesis ; Benzimidazoles/chemistry ; Benzimidazoles/pharmacology ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Clostridium Infections/drug therapy ; Crystallography, X-Ray ; DNA/chemistry ; Drug Screening Assays, Antitumor ; Humans ; Microbial Sensitivity Tests ; Models, Molecular ; Molecular Structure ; Pyridines/chemistry ; Pyridines/pharmacology |
Chemical Substances | Anti-Bacterial Agents ; Antineoplastic Agents ; Benzimidazoles ; Pyridines ; ridinilazole (06DX01190R) ; bis-benzimidazole (16656-27-2) ; DNA (9007-49-2) |
Language | English |
Publishing date | 2022-02-09 |
Publishing country | England |
Document type | Journal Article ; Review |
ZDB-ID | 1161284-8 |
ISSN | 1464-3391 ; 0968-0896 |
ISSN (online) | 1464-3391 |
ISSN | 0968-0896 |
DOI | 10.1016/j.bmc.2022.116656 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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