Please use this identifier to cite or link to this item: http://lib.jncasr.ac.in:8080/jspui/handle/10572/2493
Title: Membrane Active Vancomycin Analogues: A Strategy to Combat Bacterial Resistance
Authors: Yarlagadda, Venkateswarlu
Akkapeddi, Padma
Manjunath, Goutham B.
Haldar, Jayanta
Keywords: Medicinal Chemistry
Ala-D-Ala
Gram-Positive Bacteria
Solid-Phase Synthesis
In-Vitro Evaluation
D-Lac Binding
Staphylococcus-Aureus
Glycopeptide Antibiotics
Antibacterial Activity
Derivatives
Telavancin
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, http://dx.doi.org/10.1021/jm500270w
Journal of Medicinal Chemistry
57
11
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
URI: http://hdl.handle.net/10572/2493
ISSN: 0022-2623
Appears in Collections:Research Papers (Jayanta Haldar)

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