AI Article Synopsis
- Antibiotic-resistant superbugs like vancomycin-resistant Enterococci (VRE) and Staphylococci pose serious global health risks.
- Researchers synthesized vancomycin aglycon dimers to explore how different linkers affect their antibacterial effectiveness.
- One dimer, featuring a lipophilic moiety, was found to be about 300 times more effective than vancomycin at inhibiting VRE by enhancing its ability to bind to target peptides and disrupt cell wall production.
Article Abstract
Antibiotic-resistant superbugs such as vancomycin-resistant Enterococci (VRE) and Staphylococci have become a major global health hazard. To address this issue, we synthesized vancomycin aglycon dimers to systematically probe the impact of a linker on biological activity. A dimer having a pendant lipophilic moiety in the linker showed ∼300-fold more activity than vancomycin against VRE. The high activity of the compound is attributed to its enhanced binding affinity to target peptides which resulted in improved peptidoglycan (cell wall) biosynthesis inhibition. Therefore, our studies suggest that these compounds, prepared by using facile synthetic methodology, can be used to combat vancomycin-resistant bacterial infections.
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| http://dx.doi.org/10.1016/j.bmcl.2015.10.083 | DOI Listing |
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