5-Substituted Uridines with Activity against Gram-Positive Bacteria

ChemMedChem. 2023 Nov 2;18(21):e202300366. doi: 10.1002/cmdc.202300366. Epub 2023 Oct 4.

Abstract

The emergence of drug-resistant strains of pathogenic microorganisms necessitates the creation of new drugs. A series of uridine derivatives containing an extended substituent at the C-5 position as well as C-5 alkyloxymethyl, alkylthiomethyl, alkyltriazolylmethyl, alkylsulfinylmethyl and alkylsulfonylmethyl uridines were obtained in order to explore their antimicrobial properties and solubility. It has been shown that new ribonucleoside derivatives have an order of magnitude better solubility in water compared to their 2'-deoxy analogues and effectively inhibit the growth of a number of Gram-positive bacteria, including resistant strains of Mycobacterium smegmatis (MIC=15-200 μg/mL) and Staphylococcus aureus (MIC=25-100 μg/mL). Their activity is comparable to that of some antibiotics used in medicine.

Keywords: antibacterial agents; antifungal agents; circular dichroism; nucleosides; uridine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents* / pharmacology
  • Anti-Infective Agents* / pharmacology
  • Gram-Negative Bacteria
  • Gram-Positive Bacteria
  • Microbial Sensitivity Tests
  • Uridine / pharmacology

Substances

  • Uridine
  • Anti-Bacterial Agents
  • Anti-Infective Agents