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Carborane clusters increase the potency of bis-substituted cyclam derivatives against Mycobacterium tuberculosis.
Smith, Nicholas; Quan, Diana; Nagalingam, Gayathri; Triccas, James A; Rendina, Louis M; Rutledge, Peter J.
Afiliación
  • Smith N; School of Chemistry, The University of Sydney Sydney NSW 2006 Australia peter.rutledge@sydney.edu.au louis.rendina@sydney.edu.au +61 2 9351 5020 +61 2 9351 4781.
  • Quan D; Sydney Institute of Infectious Diseases and Charles Perkins Centre, The University of Sydney Sydney NSW 2006 Australia.
  • Nagalingam G; School of Medical Sciences, The University of Sydney Sydney NSW 2006 Australia.
  • Triccas JA; Sydney Institute of Infectious Diseases and Charles Perkins Centre, The University of Sydney Sydney NSW 2006 Australia.
  • Rendina LM; School of Medical Sciences, The University of Sydney Sydney NSW 2006 Australia.
  • Rutledge PJ; Sydney Institute of Infectious Diseases and Charles Perkins Centre, The University of Sydney Sydney NSW 2006 Australia.
RSC Med Chem ; 13(10): 1234-1238, 2022 Oct 19.
Article en En | MEDLINE | ID: mdl-36325397
Bis-substituted cyclam derivatives have recently emerged as a promising new class of antibacterial agents, displaying excellent activity against drug-resistant Mycobacterium tuberculosis (Mtb) and in vivo 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 closo-1,2-carborane or anionic, hydrophilic nido-7,8-carborane clusters display promising activity in an antibacterial assay employing the virulent Mtb strain H37Rv. The most active of these carborane derivatives exhibit MIC50 values of <1 µM, making them the most active compounds in this unique class of antibacterial cyclams reported to date.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: RSC Med Chem Año: 2022 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: RSC Med Chem Año: 2022 Tipo del documento: Article Pais de publicación: Reino Unido