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dc.contributor.authorYarlagadda, Venkateswarlu
dc.contributor.authorSarkar, Paramita
dc.contributor.authorSamaddar, Sandip
dc.contributor.authorHaldar, Jayanta
dc.date.accessioned2017-01-24T09:11:14Z-
dc.date.available2017-01-24T09:11:14Z-
dc.date.issued2016
dc.identifier.citationYarlagadda, V.; Sarkar, P.; Samaddar, S.; Haldar, J., AVancomycin Derivative with a Pyrophosphate-Binding Group: A Strategy to Combat Vancomycin-Resistant Bacteria. Angewandte Chemie-International Edition 2016, 55 (27), 7836-7840 http://dx.doi.org/10.1002/anie.201601621en_US
dc.identifier.citationAngewandte Chemie-International Editionen_US
dc.identifier.citation55en_US
dc.identifier.citation27en_US
dc.identifier.issn1433-7851
dc.identifier.urihttp://hdl.handle.net/10572/2308-
dc.descriptionRestricted Accessen_US
dc.description.abstractVancomycin, the drug of last resort for Gram-positive bacterial infections, has also been rendered ineffective by the emergence of resistance in such bacteria. To combat the threat of vancomycin-resistant bacteria (VRB), we report the development of a dipicolyl-vancomycin conjugate (Dipi-van), which leads to enhanced inhibition of cell-wall biosynthesis in VRB and displays in vitro activity that is more than two orders of magnitude higher than that of vancomycin. Conjugation of the dipicolyl moiety, which is a zinc-binding ligand, endowed the parent drug with the ability to bind to pyrophosphate groups of cell-wall lipids while maintaining the inherent binding affinity for pentapeptide termini of cell-wall precursors. Furthermore, no detectable resistance was observed after several serial passages, and the compound reduced the bacterial burden by a factor of 5 logs at 12 mg kg(-1) in a murine model of VRB kidney infection. The findings presented in this report stress the potential of our strategy to combat VRB infections.en_US
dc.description.uri1521-3773en_US
dc.description.urihttp://dx.doi.org/10.1002/anie.201601621en_US
dc.language.isoEnglishen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.rights@Wiley-V C H Verlag Gmbh, 2016en_US
dc.subjectChemistryen_US
dc.subjectantibioticsen_US
dc.subjectbacterial resistanceen_US
dc.subjectdrug designen_US
dc.subjectmultidrug-resistant bacteriaen_US
dc.subjectvancomycinen_US
dc.subjectAla-D-Alaen_US
dc.subjectGlycopeptide Antibiotics Backen_US
dc.subjectCell-Wall Synthesisen_US
dc.subjectD-Lac Bindingen_US
dc.subjectAntibacterial Activityen_US
dc.subjectStaphylococcus-Aureusen_US
dc.subjectLipid-Iien_US
dc.subjectPharmacological-Propertiesen_US
dc.subjectEscherichia-Colien_US
dc.subjectSmall Moleculesen_US
dc.titleAVancomycin Derivative with a Pyrophosphate-Binding Group: A Strategy to Combat Vancomycin-Resistant Bacteriaen_US
dc.typeArticleen_US
Appears in Collections:Research Papers (Jayanta Haldar)

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