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Carborane clusters increase the potency of bis-substituted cyclam derivatives against . | LitMetric

AI Article Synopsis

  • Bis-substituted cyclam derivatives are a new class of antibacterial agents effective against drug-resistant bacteria and have shown promising results in lab tests using zebrafish.
  • The study focuses on synthesizing new carborane derivatives that belong to this class, specifically targeting tuberculosis.
  • The most effective compounds, which combine carborane clusters with cyclam, exhibit impressive antibacterial activity, with minimum inhibitory concentration (MIC) values of less than 1 μM, marking them as the strongest in their group thus far.

Article Abstract

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 <1 μM, making them the most active compounds in this unique class of antibacterial cyclams reported to date.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9579921PMC
http://dx.doi.org/10.1039/d2md00150kDOI Listing

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