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Thiol- and Disulfide-Containing Vancomycin Derivatives Against Bacterial Resistance and Biofilm Formation


Shchelik, Inga S; Gademann, Karl (2021). Thiol- and Disulfide-Containing Vancomycin Derivatives Against Bacterial Resistance and Biofilm Formation. ACS Medicinal Chemistry Letters, 12(12):1898-1904.

Abstract

Antibiotic-resistant and biofilm-associated infections constitute a rapidly growing issue. Use of the last resort antibiotic vancomycin is under threat, due to the increasing appearance of vancomycin resistant bacteria as well as the formation of biofilms. Herein, we report a series of novel vancomycin derivatives carrying thiol- and disulfide-containing moieties. The new compounds exhibited enhanced antibacterial activity against a broad range of bacterial strains, including vancomycin resistant microbes and Gram-negative bacteria. Moreover, all obtained derivatives demonstrated improved antibiofilm formation activity against VanB resistant Enterococcus compared to vancomycin. This work established a promising strategy for combating drug-resistant bacterial infections or disrupting biofilm formation and advances the knowledge on structural optimization of antibiotics with sulfur-containing modifications.

Abstract

Antibiotic-resistant and biofilm-associated infections constitute a rapidly growing issue. Use of the last resort antibiotic vancomycin is under threat, due to the increasing appearance of vancomycin resistant bacteria as well as the formation of biofilms. Herein, we report a series of novel vancomycin derivatives carrying thiol- and disulfide-containing moieties. The new compounds exhibited enhanced antibacterial activity against a broad range of bacterial strains, including vancomycin resistant microbes and Gram-negative bacteria. Moreover, all obtained derivatives demonstrated improved antibiofilm formation activity against VanB resistant Enterococcus compared to vancomycin. This work established a promising strategy for combating drug-resistant bacterial infections or disrupting biofilm formation and advances the knowledge on structural optimization of antibiotics with sulfur-containing modifications.

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Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:07 Faculty of Science > Department of Chemistry
Dewey Decimal Classification:540 Chemistry
Scopus Subject Areas:Life Sciences > Biochemistry
Life Sciences > Drug Discovery
Physical Sciences > Organic Chemistry
Uncontrolled Keywords:vancomycin, antibiotic resistance, bacterial biofilm, antibiotics, disulfides
Language:English
Date:9 December 2021
Deposited On:17 Jan 2022 16:14
Last Modified:26 Jun 2024 01:49
Publisher:American Chemical Society (ACS)
ISSN:1948-5875
OA Status:Green
Publisher DOI:https://doi.org/10.1021/acsmedchemlett.1c00455
Project Information:
  • : FunderSNSF
  • : Grant ID200021_182043
  • : Project TitleMechanism-Based Design, Synthesis, Biological Evaluation, and Delivery of Next-Generation Antibiotics
  • : FunderStaatssekretariat f??r Bildung, Forschung und Innovation
  • : Grant ID
  • : Project Title
  • Content: Accepted Version
  • Language: English