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Title: Lipophilic vancomycin aglycon dimer with high activity against vancomycin-resistant bacteria
Authors: Yarlagadda, Venkateswarlu
Sarkar, Paramita
Manjunath, Goutham B.
Haldar, Jayanta
Keywords: Medicinal Chemistry
Chemistry, Organic
Antibiotic resistance
Vancomycin-resistant bacteria
Cell wall biosynthesis inhibition
Antibacterial activity
Glycopeptide Antibiotic-Activity
In-Vivo Efficacy
Antibacterial Activity
Issue Date: 2015
Publisher: Pergamon-Elsevier Science Ltd
Citation: Bioorganic & Medicinal Chemistry Letters
Yarlagadda, V.; Sarkar, P.; Manjunath, G. B.; Haldar, J., Lipophilic vancomycin aglycon dimer with high activity against vancomycin-resistant bacteria. Bioorganic & Medicinal Chemistry Letters 2015, 25 (23), 5477-5480.
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 similar to 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. (C) 2015 Elsevier Ltd. All rights reserved.
Description: Restricted access
ISSN: 0960-894X
Appears in Collections:Research Papers (Jayanta Haldar)

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