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dc.contributor.authorYarlagadda, Venkateswarlu
dc.contributor.authorAkkapeddi, Padma
dc.contributor.authorManjunath, Goutham B.
dc.contributor.authorHaldar, Jayanta
dc.date.accessioned2017-02-21T08:57:42Z-
dc.date.available2017-02-21T08:57:42Z-
dc.date.issued2014
dc.identifier.citationYarlagadda, 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/jm500270wen_US
dc.identifier.citationJournal of Medicinal Chemistryen_US
dc.identifier.citation57en_US
dc.identifier.citation11en_US
dc.identifier.issn0022-2623
dc.identifier.urihttp://hdl.handle.net/10572/2493-
dc.descriptionRestricted Accessen_US
dc.description.abstractThe 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.uri1520-4804en_US
dc.description.urihttp://dx.doi.org/10.1021/jm500270wen_US
dc.language.isoEnglishen_US
dc.publisherAmerican Chemical Societyen_US
dc.rights@American Chemical Society, 2014en_US
dc.subjectMedicinal Chemistryen_US
dc.subjectAla-D-Alaen_US
dc.subjectGram-Positive Bacteriaen_US
dc.subjectSolid-Phase Synthesisen_US
dc.subjectIn-Vitro Evaluationen_US
dc.subjectD-Lac Bindingen_US
dc.subjectStaphylococcus-Aureusen_US
dc.subjectGlycopeptide Antibioticsen_US
dc.subjectAntibacterial Activityen_US
dc.subjectDerivativesen_US
dc.subjectTelavancinen_US
dc.titleMembrane Active Vancomycin Analogues: A Strategy to Combat Bacterial Resistanceen_US
dc.typeArticleen_US
Appears in Collections:Research Papers (Jayanta Haldar)

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