<p>The reactions of substituted 1,4-naphthoquinones with ethanolamine or <i>N</i>-acetylcysteamine gave acyclic products, conditions for the cyclization of which into linear tricyclic oxazines and thiazines were found. The cytotoxic, antimicrobial, and neuroprotective activities of the new compounds were evaluated. The acyclic derivatives of ethanolamine and cysteamine exhibited high antimicrobial activity and cytotoxicity. Tricyclic naphthooxazines and naphthothiazines showed potential as compounds with neuroprotective activity.</p>

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Synthesis of tricyclic oxazine and thiazine fused 1,4-naphthoquinone derivatives based on ethanolamine and cysteamine. Primary evaluation of cytotoxic, antimicrobial, and neuroprotective activities

  • Yu. E. Sabutski,
  • E. S. Menchinskaya,
  • E. A. Pislyagin,
  • E. A. Chingizova,
  • D. L. Aminin,
  • S. G. Polonik

摘要

The reactions of substituted 1,4-naphthoquinones with ethanolamine or N-acetylcysteamine gave acyclic products, conditions for the cyclization of which into linear tricyclic oxazines and thiazines were found. The cytotoxic, antimicrobial, and neuroprotective activities of the new compounds were evaluated. The acyclic derivatives of ethanolamine and cysteamine exhibited high antimicrobial activity and cytotoxicity. Tricyclic naphthooxazines and naphthothiazines showed potential as compounds with neuroprotective activity.