<p>In this work, stable chemical precursors (3,5-DTBC) and alkylated derivatives were synthesized through strategic modifications guided by the redox and chelation properties of catechol. Leveraging the molecular principle that fusing two bioactive components often yields synergistic effects, catechol — a polyphenol with broad biological activities — was integrated into the nitrogen-containing heterocyclic core structure, imidazolidine-2,4-dione, to design a novel class of hybrid compounds (<b>7a</b>–<b>q</b>) with diverse pharmacological profiles. The primary objective was to explore efficient synthetic routes, characterize structures via physicochemical analyses, and possible evaluate cytotoxicity and AT1-inhibitory activity in vitro.</p>

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Synthesis and in vitro study of a novel catechol with a hydantoin core

  • Xiumei Bai,
  • Daria A. Ipatova,
  • Dmitry A. Skvortsov,
  • Vyacheslav A. Chertkov,
  • Boris N. Tarasevich,
  • Jinlei Bian,
  • Yury V. Timchenko,
  • Igor A. Rodin,
  • Victor A. Tafeenko,
  • Dmitry S. Yakovlev,
  • Alexander A. Spasov,
  • Raul I. Musaev,
  • Nataliya A. Gurova,
  • Jiayue Gao,
  • Elena R. Milaeva,
  • Elena K. Beloglazkina,
  • Alexander V. Finko

摘要

In this work, stable chemical precursors (3,5-DTBC) and alkylated derivatives were synthesized through strategic modifications guided by the redox and chelation properties of catechol. Leveraging the molecular principle that fusing two bioactive components often yields synergistic effects, catechol — a polyphenol with broad biological activities — was integrated into the nitrogen-containing heterocyclic core structure, imidazolidine-2,4-dione, to design a novel class of hybrid compounds (7aq) with diverse pharmacological profiles. The primary objective was to explore efficient synthetic routes, characterize structures via physicochemical analyses, and possible evaluate cytotoxicity and AT1-inhibitory activity in vitro.