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dc.contributor.authorKonai, Mohini M.
dc.contributor.authorGhosh, Chandradhish
dc.contributor.authorYarlagadda, Venkateswarlu
dc.contributor.authorSamaddar, Sandip
dc.contributor.authorHaldar, Jayanta
dc.date.accessioned2017-02-21T08:57:42Z-
dc.date.available2017-02-21T08:57:42Z-
dc.date.issued2014
dc.identifier.citationKonai, MM; Ghosh, C; Yarlagadda, V; Samaddar, S; Haldar, J, Membrane Active Phenylalanine Conjugated Lipophilic Norspermidine Derivatives with Selective Antibacterial Activity. Journal of Medicinal Chemistry 2014, 57 (22) 9409-9423, http://dx.doi.org/10.1021/jm5013566en_US
dc.identifier.citationJournal of Medicinal Chemistryen_US
dc.identifier.citation57en_US
dc.identifier.citation22en_US
dc.identifier.issn0022-2623
dc.identifier.urihttp://hdl.handle.net/10572/2492-
dc.descriptionRestricted Accessen_US
dc.description.abstractNatural and synthetic membrane active antibacterial agents offer hope as potential solutions to the problem of bacterial resistance as the membrane-active nature imparts low propensity for the development of resistance. In this report norspermidine based antibacterial molecules were developed that displayed excellent antibacterial activity against various wild-type bacteria (Gram-positive and Gram-negative) and drug-resistant bacteria (methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and beta-lactam-resistant Klebsiella pneumoniae). In a novel structureactivity relationship study it has been shown how incorporation of an aromatic amino acid drastically improves selective antibacterial activity. Additionally, the effect of stereochemistry on activity, toxicity, and plasma stability has also been studied. These rapidly bactericidal, membrane active antibacterial compounds do not trigger development of resistance in bacteria and hence bear immense potential as therapeutic agents to tackle multidrug resistant bacterial infections.en_US
dc.description.uri1520-4804en_US
dc.description.urihttp://dx.doi.org/10.1021/jm5013566en_US
dc.language.isoEnglishen_US
dc.publisherAmerican Chemical Societyen_US
dc.rights@American Chemical Society, 2014en_US
dc.subjectMedicinal Chemistryen_US
dc.subjectHelical Antimicrobial Peptidesen_US
dc.subjectDe-Novo Designen_US
dc.subjectPeptoid Mimicsen_US
dc.subjectBeta-Peptidesen_US
dc.subjectLipopeptidesen_US
dc.subjectPeptidomimeticsen_US
dc.subjectResistanceen_US
dc.subjectBacteriaen_US
dc.subjectAgentsen_US
dc.subjectAmphiphilesen_US
dc.titleMembrane Active Phenylalanine Conjugated Lipophilic Norspermidine Derivatives with Selective Antibacterial Activityen_US
dc.typeArticleen_US
Appears in Collections:Research Papers (Jayanta Haldar)

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