Carborane clusters increase the potency of bis-substituted cyclam derivatives against Mycobacterium tuberculosis

Bis-substituted cyclam derivatives have recently emerged as a promising new class of antibacterial agents, displaying excellent activity against drug-resistant ( ) and efficacy in a zebrafish assay. Herein we report the synthesis and biological activity of new carborane derivatives within this class...

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Bibliographic Details
Published in:MedChemComm 2022-10, Vol.13 (10), p.1234-1238
Main Authors: Smith, Nicholas, Quan, Diana, Nagalingam, Gayathri, Triccas, James A, Rendina, Louis M, Rutledge, Peter J
Format: Article
Language:English
Subjects:
Antibacterial agents
Biological activity
Carborane
Chemistry
Clusters
Drug resistance
Hydrophobicity
Mycobacterium tuberculosis
Substitutes
Tuberculosis
Zebrafish
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Summary:Bis-substituted cyclam derivatives have recently emerged as a promising new class of antibacterial agents, displaying excellent activity against drug-resistant ( ) and efficacy in a zebrafish assay. Herein we report the synthesis and biological activity of new carborane derivatives within this class of antitubercular compounds. The resulting carborane-cyclam conjugates incorporating either hydrophobic -1,2-carborane or anionic, hydrophilic -7,8-carborane clusters display promising activity in an antibacterial assay employing the virulent strain H37Rv. The most active of these carborane derivatives exhibit MIC values of
ISSN:2632-8682
2040-2503
2632-8682
2040-2511
DOI:10.1039/d2md00150k