<p>In order to improve the solubility of 3,5-bis(arylidene)piperidin-4-ones with various substituents in the benzene ring, the corresponding 2-(2-methoxyethoxy)ethyl-[3,5-bis-(arylidene)-4-oxo-1-piperidinyl]acetates were obtained. Evaluation of their physicochemical characteristics <i>in silico</i> showed that the inclusion of 2-(2-methoxyethoxy)ethanol with an OMe terminal group in the piperidone molecules improves its pharmacokinetic characteristics and, as a consequence, its solubility in aqueous media and cytotoxic profile.</p>

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Synthesis of 3,5-bis(arylidene)piperidin-4-ones with a polyester chain as an approach to obtaining molecules with improved solubility

  • Yu. R. Aleksandrova,
  • M. E. Neganova,
  • I. A. Shagina,
  • A. S. Kolesnikov,
  • A. S. Tapalova,
  • V. K. Brel

摘要

In order to improve the solubility of 3,5-bis(arylidene)piperidin-4-ones with various substituents in the benzene ring, the corresponding 2-(2-methoxyethoxy)ethyl-[3,5-bis-(arylidene)-4-oxo-1-piperidinyl]acetates were obtained. Evaluation of their physicochemical characteristics in silico showed that the inclusion of 2-(2-methoxyethoxy)ethanol with an OMe terminal group in the piperidone molecules improves its pharmacokinetic characteristics and, as a consequence, its solubility in aqueous media and cytotoxic profile.