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Benzocaine-N-acylindoline conjugates: synthesis and antiviral activity against Coxsackievirus B3

  • Alexandrina S. Volobueva,
  • Anton A. Shetnev,
  • Mikhail G. Mikhalski,
  • Valeria A. Panova,
  • Darina D. Barkhatova,
  • Ekaterina D. Korshunova,
  • Sergey A. Ivanovskiy,
  • Vladimir V. Zarubaev,
  • Sergey V. Baykov

摘要

Indoline-5-sulfonamide derivatives of benzocaine have been synthesized using a sequence of three reactions: N-acylation, sulfochlorination, sulfonamidation, and their antienteroviral activity has been evaluated. Two compounds, namely, ethyl 4-((1-(cyclobutanecarbonyl)indoline)-5-sulfonamido)benzoate and ethyl 4-((1-benzoylindoline)-5-sulfonamido)benzoate exhibited a medium level of activity against coxsackievirus B3 (Nancy strain) in vitro. Their antiviral potential is exerted upon prophylactic application when added to cell culture before infection with the virus.