<p>Analogs of the alkaloids polycarpine and polycarpaurine C, metabolites of marine ascidians of the genus <i>Polycarpa</i>, were synthesized. Their cytotoxic and antimicrobial activities were comparatively analyzed. A chloro-containing analog of polycarpaurine C was shown to exhibit high antibacterial activity against <i>Staphylococcus aureus</i> and <i>Escherichia coli</i> superior to that of gentamicin. Polycarpaurine C and its thioanalogs strongly inhibited biofilm formation by the studied microorganisms.</p>

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Antimicrobial and Cytotoxic Activity of Imidazole and Thiazole Analogs of Polycarpine and Polycarpaurine C

  • Yu. E. Sabutski,
  • S. M. Kovach,
  • N. N. Balaneva,
  • K. L. Borisova,
  • E. A. Chingizova,
  • E. S. Menchinskaya,
  • A. L. Burylova,
  • A. R. Chingizov,
  • B. P. Mashnev,
  • D. N. Pelageev

摘要

Analogs of the alkaloids polycarpine and polycarpaurine C, metabolites of marine ascidians of the genus Polycarpa, were synthesized. Their cytotoxic and antimicrobial activities were comparatively analyzed. A chloro-containing analog of polycarpaurine C was shown to exhibit high antibacterial activity against Staphylococcus aureus and Escherichia coli superior to that of gentamicin. Polycarpaurine C and its thioanalogs strongly inhibited biofilm formation by the studied microorganisms.