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Abstract <p><b>Objective:</b> Nucleoside derivatives are widely used for drug development. We previously obtained <i>N</i><sup>4</sup>-alkyl derivatives of 2′-deoxycytidine and cytidine, which showed significant inhibitory activity against Gram-positive bacteria, but the exact mechanism of their action remains unexplained at present. One of the methods for elucidating the mechanisms of action of biologically active molecules and, consequently, for increasing their therapeutic effectiveness is identifying the subcellular localization of low-molecular-weight compounds. <b>Methods:</b> In this study, new derivatives of <i>N</i><sup>4</sup>-dodecyl-5-methyl-2′-deoxycytidine containing terminal amino groups at the end of an alkyl linker have been synthesized. It is shown that they are convenient synthons for the subsequent introduction of dansyl fluorophore groups. <b>Results and Discussion:</b> One of the <i>N</i><sup>4</sup>-ω-dansylaminoalkyl derivatives has shown moderate antibacterial activity against the <i>Mycobacterium smegmatis</i> strain. This derivative can be used to study the subcellular localization. <b>Conclusions:</b> The synthesized derivatives have potential for further research, particularly in studying their subcellular localization.</p>

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N4-(ω-Aminoalkyl)- and N4-(ω-Dansylaminoalkyl)-5-methyl-2′-deoxycytidines

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • D. A. Makarov,
  • M. V. Jasko,
  • I. L. Karpenko,
  • Y. V. Tkachev,
  • B. F. Vasilyeva,
  • O. V. Efremenkova,
  • S. N. Kochetkov,
  • L. A. Alexandrova

摘要

Abstract

Objective: Nucleoside derivatives are widely used for drug development. We previously obtained N4-alkyl derivatives of 2′-deoxycytidine and cytidine, which showed significant inhibitory activity against Gram-positive bacteria, but the exact mechanism of their action remains unexplained at present. One of the methods for elucidating the mechanisms of action of biologically active molecules and, consequently, for increasing their therapeutic effectiveness is identifying the subcellular localization of low-molecular-weight compounds. Methods: In this study, new derivatives of N4-dodecyl-5-methyl-2′-deoxycytidine containing terminal amino groups at the end of an alkyl linker have been synthesized. It is shown that they are convenient synthons for the subsequent introduction of dansyl fluorophore groups. Results and Discussion: One of the N4-ω-dansylaminoalkyl derivatives has shown moderate antibacterial activity against the Mycobacterium smegmatis strain. This derivative can be used to study the subcellular localization. Conclusions: The synthesized derivatives have potential for further research, particularly in studying their subcellular localization.