Abstract <p><b>Objective:</b> Methods for obtaining new derivatives of <i>N</i><sup>4</sup>-dodecylamino-2′-deoxycytidine and cytidine have been developed with the aim to prepare convenient synthons for the introduction of tags (above all, fluorescent dyes) into biopolymers and cells for further study of their cellular localization. <b>Methods:</b> The new derivatives contain 5-ethynyl, 5-(prop-2-in-1-yl)oxymethyl, or 5′-azido groups necessary for the introduction of dyes <i>in vitro</i> using click chemistry methods. <b>Results and Discussion:</b> The obtained compounds, like <i>N</i><sup>4</sup>-dodecylamino-2′-deoxycytidine, showed significant antibacterial activity against Gram-positive bacteria. <b>Conclusions:</b> The new nucleosides can be used for visualizing their subcellular localization, which may help in determining the potential mechanism of action of antibacterial agents of this type.</p>

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Synthesis and Antibacterial Activity of Ethynyl and Azido Derivatives of N4-Dodecylamino-2′-deoxycytidine

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

摘要

Abstract

Objective: Methods for obtaining new derivatives of N4-dodecylamino-2′-deoxycytidine and cytidine have been developed with the aim to prepare convenient synthons for the introduction of tags (above all, fluorescent dyes) into biopolymers and cells for further study of their cellular localization. Methods: The new derivatives contain 5-ethynyl, 5-(prop-2-in-1-yl)oxymethyl, or 5′-azido groups necessary for the introduction of dyes in vitro using click chemistry methods. Results and Discussion: The obtained compounds, like N4-dodecylamino-2′-deoxycytidine, showed significant antibacterial activity against Gram-positive bacteria. Conclusions: The new nucleosides can be used for visualizing their subcellular localization, which may help in determining the potential mechanism of action of antibacterial agents of this type.