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dc.contributor.authorKonai, Mohini M.
dc.contributor.authorAdhikary, Utsarga
dc.contributor.authorSamaddar, Sandip
dc.contributor.authorGhosh, Chandradhish
dc.contributor.authorHaldar, Jayanta
dc.identifier.citationBioconjugate Chemistryen_US
dc.identifier.citationKonai, M. M.; Adhikary, U.; Samaddar, S.; Ghosh, C.; Haldar, J., Structure-Activity Relationship of Amino Acid Tunable Lipidated Norspermidine Conjugates: Disrupting Biofilms with Potent Activity against Bacterial Persisters. Bioconj. Chem. 2015, 26 (12), 2442-2453.en_US
dc.descriptionRestricted accessen_US
dc.description.abstractThe emergence of bacterial resistance and biofilm associated infections has created a challenging situation in global health. In this present state of affairs where conventional antibiotics are falling short of being able to provide a solution to these problems, development of novel antibacterial compounds possessing the twin prowess of antibacterial and antibiofilm efficacy is imperative. Herein, we report a library of amino acid tunable lipidated norspermidine conjugates that were prepared by conjugating both amino acids and fatty acids with the amine functionalities of norspermidine through amide bond formation. These lipidated conjugates displayed potent antibacterial activity against various planktonic Gram-positive and Gram-negative bacteria including drug-resistant superbugs such as methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and beta-lactam-resistant Klebsiella pneumoniae. This class of nontoxic and fast-acting antibacterial molecules (capable of killing bacteria within 15 min) did not allow bacteria to develop resistance against them after several passages. Most importantly, an optimized compound in the series was also capable of killing metabolically inactive persisters and stationary phase bacteria. Additionally, this compound was capable of disrupting the preformed biofilms of S. aureus and E. coli. Therefore, this class of antibacterial conjugates have potential in tackling the challenging situation posed by both bacterial resistance as well as drug tolerance due to biofilm formation.en_US
dc.publisherAmerican Chemical Societyen_US
dc.rights?American Chemical Society, 2015en_US
dc.subjectBiochemical Research Methodsen_US
dc.subjectBiochemistry & Molecular Biologyen_US
dc.subjectChemistry, Organicen_US
dc.subjectPseudomonas-Aeruginosa Biofilmsen_US
dc.subjectHelical Antimicrobial Peptidesen_US
dc.subjectAntibacterial Activityen_US
dc.subjectCationic Amphiphilesen_US
dc.titleStructure-Activity Relationship of Amino Acid Tunable Lipidated Norspermidine Conjugates: Disrupting Biofilms with Potent Activity against Bacterial Persistersen_US
Appears in Collections:Research Papers (Jayanta Haldar)

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