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<p>The emergence of drug resistance in pathogenic strains and the associated rise in mortality have driven the need for new, highly effective antimycotics based on azole derivatives. New chiral hybrids comprising a 1-(2,4-dichlorophenyl)-2-(1<i>H</i>-1,2,4-triazol-1-yl)ethyl moiety and a monoterpene thiol with a 1,3-dioxolan-4-ylmethyl linker, structurally similar to the itraconazole and ketoconazole pharmacophores, were synthesized. The hybrids demonstrated high antifungal activity against both fluconazole-susceptible and fluconazole-resistant <i>Candida albicans</i> strains. The affinity of the synthesized compounds for a fungal enzyme, lanosterol-14α-demethylase (CYP51), was evaluated. This enzyme catalyzes a key step in the biosynthesis of ergosterol, a steroidal component that plays a critical role in maintaining the structural integrity and functional activity of fungal cell membranes.</p>

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Synthesis and evaluation of antifungal activity of novel chiral 1,2,4-triazole derivatives bearing monoterpenylsulfanyl moieties

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • P. V. Gribkov,
  • D. V. Sudarikov,
  • S. A. Lisovskaya,
  • L. E. Nikitina,
  • A. R. Kayumov,
  • S. A. Rubtsova,
  • A. V. Kutchin

摘要

The emergence of drug resistance in pathogenic strains and the associated rise in mortality have driven the need for new, highly effective antimycotics based on azole derivatives. New chiral hybrids comprising a 1-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethyl moiety and a monoterpene thiol with a 1,3-dioxolan-4-ylmethyl linker, structurally similar to the itraconazole and ketoconazole pharmacophores, were synthesized. The hybrids demonstrated high antifungal activity against both fluconazole-susceptible and fluconazole-resistant Candida albicans strains. The affinity of the synthesized compounds for a fungal enzyme, lanosterol-14α-demethylase (CYP51), was evaluated. This enzyme catalyzes a key step in the biosynthesis of ergosterol, a steroidal component that plays a critical role in maintaining the structural integrity and functional activity of fungal cell membranes.