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<p>An approach to the synthesis of hybrid multitarget compounds based on 4-amino-2,3-polymethylenequinolines (analogs of the drug tacrine) with different sizes of the aliphatic ring, which are coupled with a vanillin fragment as an antioxidant pharmacophore, was developed. The coupling was accomplished through the amide bond using an alkylamine linker. The synthesized hybrid compounds were found to highly efficiently inhibit cholinesterases, showing selectivity for butyrylcholinesterase, displace propidium cation from the peripheral anionic site of acetylcholinesterase (AChE), <i>i.e.</i>, they are able to block AChE-induced aggregation of β-amyloid, and demonstrate high antioxidant activity. Compound <b>9c</b> with a largest aliphatic ring size (C<sub>7</sub>), which exerted a multitarget effect on the studied targets, can be used as a potential candidate for further research on the extention of the spectrum of its biological activity.</p>

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New multitarget derivatives of tacrine and its analogs containing a vanillin moiety as an antioxidant pharmacophore

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • I. V. Serkov,
  • A. N. Proshin,
  • N. P. Boltneva,
  • N. V. Kovaleva,
  • E. V. Rudakova,
  • G. F. Makhaeva

摘要

An approach to the synthesis of hybrid multitarget compounds based on 4-amino-2,3-polymethylenequinolines (analogs of the drug tacrine) with different sizes of the aliphatic ring, which are coupled with a vanillin fragment as an antioxidant pharmacophore, was developed. The coupling was accomplished through the amide bond using an alkylamine linker. The synthesized hybrid compounds were found to highly efficiently inhibit cholinesterases, showing selectivity for butyrylcholinesterase, displace propidium cation from the peripheral anionic site of acetylcholinesterase (AChE), i.e., they are able to block AChE-induced aggregation of β-amyloid, and demonstrate high antioxidant activity. Compound 9c with a largest aliphatic ring size (C7), which exerted a multitarget effect on the studied targets, can be used as a potential candidate for further research on the extention of the spectrum of its biological activity.