5‐Substituted Uridines with Activity against Gram‐Positive Bacteria-Reference-Cited by-同舟云学术

5‐Substituted Uridines with Activity against Gram‐Positive Bacteria

Published:2023-10-04 Issue:21 Volume:18 Page:
ISSN:1860-7179
Container-title:ChemMedChem
language:en
Short-container-title:ChemMedChem

Author:

Makarov Dmitry A.¹^ORCID,Negrya Sergey D.¹^ORCID,Jasko Maxim V.¹^ORCID,Karpenko Inna L.¹^ORCID,Solyev Pavel N.¹^ORCID,Chekhov Vladimir O.¹^ORCID,Kaluzhny Dmitry N.¹^ORCID,Efremenkova Olga V.²^ORCID,Vasilyeva Byazilya F.²^ORCID,Chizhov Alexander O.³^ORCID,Avdanina Darya A.⁴^ORCID,Zhgun Alexander A.⁴^ORCID,Kochetkov Sergey N.¹^ORCID,Alexandrova Liudmila A.¹^ORCID

Affiliation:

1. Engelhardt Institute of Molecular Biology RAS 32 Vavilov str. Moscow 119991 Russia

2. Gause Institute of New Antibiotics 11 Bol'shaya Pirogovskaya Moscow 119021 Russia

3. Zelinsky Institute of Organic Chemistry RAS 47 Leninsky Ave. Moscow 119991 Russia

4. Research Center of Biotechnology RAS 33 Leninsky Ave. Moscow 119071 Russia

Abstract

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.

Funder

Russian Science Foundation

Ministry of Education and Science of the Russian Federation

Publisher

Wiley

Subject

Organic Chemistry,General Pharmacology, Toxicology and Pharmaceutics,Molecular Medicine,Drug Discovery,Biochemistry,Pharmacology

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