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Membrane Active Vancomycin Analogues: A Strategy to Combat Bacterial Resistance

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dc.contributor.author Yarlagadda, Venkateswarlu
dc.contributor.author Akkapeddi, Padma
dc.contributor.author Manjunath, Goutham B.
dc.contributor.author Haldar, Jayanta
dc.date.accessioned 2017-02-21T08:57:42Z
dc.date.available 2017-02-21T08:57:42Z
dc.date.issued 2014
dc.identifier.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 en_US
dc.identifier.citation Journal of Medicinal Chemistry en_US
dc.identifier.citation 57 en_US
dc.identifier.citation 11 en_US
dc.identifier.issn 0022-2623
dc.identifier.uri https://libjncir.jncasr.ac.in/xmlui/10572/2493
dc.description Restricted Access en_US
dc.description.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. en_US
dc.description.uri 1520-4804 en_US
dc.description.uri http://dx.doi.org/10.1021/jm500270w en_US
dc.language.iso English en_US
dc.publisher American Chemical Society en_US
dc.rights @American Chemical Society, 2014 en_US
dc.subject Medicinal Chemistry en_US
dc.subject Ala-D-Ala en_US
dc.subject Gram-Positive Bacteria en_US
dc.subject Solid-Phase Synthesis en_US
dc.subject In-Vitro Evaluation en_US
dc.subject D-Lac Binding en_US
dc.subject Staphylococcus-Aureus en_US
dc.subject Glycopeptide Antibiotics en_US
dc.subject Antibacterial Activity en_US
dc.subject Derivatives en_US
dc.subject Telavancin en_US
dc.title Membrane Active Vancomycin Analogues: A Strategy to Combat Bacterial Resistance en_US
dc.type Article en_US


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