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<p>The one-pot synthesis of novel molecular hybrids incorporating pseudopeptide and steroidal moieties is described. For this, an efficient conjugation approach based on the Ugi four-component reaction (Ugi-4CR) was implemented for the ligation of amines or L-aminoacids to 3-oxolithocholic acid. Compounds <b>3</b> and <b>4</b> showed a more pronounced <i>α</i>-glucosidase inhibitory activity than acarbose in vitro with IC<sub>50</sub> values 16.30 and 11.04 μM.</p>

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An Approach to 3-Oxolithocholic Acid α-Acylaminocarboxamides with α-Glucosidase Inhibitory Activity

  • 期刊论文

  • 发表日期：

    2026年1月1日

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  • A. A. Smirnova,
  • E. V. Tretyakova,
  • H. T. T. Nguyen,
  • O. B. Kazakova

摘要

The one-pot synthesis of novel molecular hybrids incorporating pseudopeptide and steroidal moieties is described. For this, an efficient conjugation approach based on the Ugi four-component reaction (Ugi-4CR) was implemented for the ligation of amines or L-aminoacids to 3-oxolithocholic acid. Compounds 3 and 4 showed a more pronounced α-glucosidase inhibitory activity than acarbose in vitro with IC50 values 16.30 and 11.04 μM.