Please use this identifier to cite or link to this item:
Title: Membrane Active Vancomycin Analogues: A Strategy to Combat Bacterial Resistance
Authors: Yarlagadda, Venkateswarlu
Akkapeddi, Padma
Manjunath, Goutham B.
Haldar, Jayanta
Keywords: Medicinal Chemistry
Gram-Positive Bacteria
Solid-Phase Synthesis
In-Vitro Evaluation
D-Lac Binding
Glycopeptide Antibiotics
Antibacterial Activity
Issue Date: 2014
Publisher: American Chemical Society
Citation: Yarlagadda, V; Akkapeddi, P; Manjunath, GB; Haldar, J, Membrane Active Vancomycin Analogues: A Strategy to Combat Bacterial Resistance. Journal of Medicinal Chemistry 2014, 57 (11) 4558-4568,
Journal of Medicinal Chemistry
Abstract: The alarming growth of antibiotic resistant superbugs such as vancomycin-resistant Enterococci and Staphylococci has become a major global health hazard. To address this issue, we report the development of lipophilic cationic vancomycin analogues possessing excellent antibacterial activity against several drug-resistant strains. Compared to vancomycin, efficacy greater than 1000-fold was demonstrated against vancomycin-resistant Enterococci (VRE). Significantly, unlike vancomycin, these compounds were shown to be bactericidal at low concentrations and did not induce bacterial resistance. An optimized compound in the series, compared to vancomycin, showed higher activity in methicillin-resistant Staphylococcus aureus (MRSA) infected mouse model and exhibited superior antibacterial activity in whole blood with no observed toxicity. The remarkable activity of these compounds is attributed to the incorporation of a new membrane disruption mechanism into vancomycin and opens up a great opportunity for the development of novel antibiotics.
Description: Restricted Access
ISSN: 0022-2623
Appears in Collections:Research Papers (Jayanta Haldar)

Files in This Item:
File Description SizeFormat 
  Restricted Access
2.69 MBAdobe PDFView/Open Request a copy

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.