5‐Substituted Uridines with Activity against Gram‐Positive Bacteria

• DOI: 10.1002/cmdc.202300366
• Publication Date: 2023-09-14T17:45:30Z
• Authors: Dmitry A. Makarov; Sergey D. Negrya; Maxim V. Jasko; Inna L. Karpenko; Pavel N. Solyev; Vladimir O. Chekhov; Dmitry N. Kaluzhny; Olga V. Efremenkova; Byazilya F. Vasil...; Alexander O. Chizhov; Darya A. Avdanina; Alexander A. Zhgun; Sergey N. Kochetkov; Liudmila A. Alexa...
• Keywords: Anti-Infective Agents; Gram-Negative Bacteria; Microbial Sensitivity Tests; Gram-Positive Bacteria; Uridine; 3. Good health; Anti-Bacterial Agents

AbstractThe 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.