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<p>In present work a series of sulfonamide-containing 3-hydroxy-2-oxindoles was designed and synthesized via condensation of isatins with malonic or cyanoacetic acids and their biological activity was evaluated. All synthesized compounds are effective nanomolar carbonic anhydrase II inhibitors, the best inhibitors <b>4a</b> and <b>4</b> <b>h</b> showed IC<sub>50</sub> 20 and 28 nM, respectively. Two animal models (rats, rabbits) were used to study the influence of compounds on intraocular pressure (IOP) in vivo. Instillation of 0.1% aq. solution of compounds <b>4a</b>, <b>4</b> <b>h</b> and <b>5i</b> showed 17, 21 and 25% decrease in IOP in rabbits, respectively. At the same time instillation of 0.4% aq. solution of almost all compounds caused a moderate IOP decrease in rats, with compounds <b>4i</b> and <b>5i</b> have shown the best effect (30 and 34% ΔIOP, respectively). All synthesized compounds showed moderate Fe<sup>2+</sup>-induced lipid peroxidation inhibition in rat brain homogenate and do not exhibit mitochondrial toxicity.</p><p></p>

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Sulfonamide-substituted oxindoles as inhibitors of carbonic anhydrase II with potential antiglaucoma activity

  • 期刊论文

  • 发表日期：

    2025年11月24日

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  • Natalia Lozinskaya,
  • Nikita Krylov,
  • Daria Vinogradova,
  • Alexander Efremov,
  • Olga Beznos,
  • Mariia Salykina,
  • Lyudmila Naumenko,
  • Alena Taran,
  • Alina Cheban’ko,
  • Ivan Veselov,
  • Sergey Sosonyuk,
  • Alexander Spasov,
  • Elena Shevtsova

摘要

In present work a series of sulfonamide-containing 3-hydroxy-2-oxindoles was designed and synthesized via condensation of isatins with malonic or cyanoacetic acids and their biological activity was evaluated. All synthesized compounds are effective nanomolar carbonic anhydrase II inhibitors, the best inhibitors 4a and 4 h showed IC50 20 and 28 nM, respectively. Two animal models (rats, rabbits) were used to study the influence of compounds on intraocular pressure (IOP) in vivo. Instillation of 0.1% aq. solution of compounds 4a, 4 h and 5i showed 17, 21 and 25% decrease in IOP in rabbits, respectively. At the same time instillation of 0.4% aq. solution of almost all compounds caused a moderate IOP decrease in rats, with compounds 4i and 5i have shown the best effect (30 and 34% ΔIOP, respectively). All synthesized compounds showed moderate Fe2+-induced lipid peroxidation inhibition in rat brain homogenate and do not exhibit mitochondrial toxicity.