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Structure-Activity Relationship of Amino Acid Tunable Lipidated Norspermidine Conjugates: Disrupting Biofilms with Potent Activity against Bacterial Persisters

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dc.contributor.author Konai, Mohini M.
dc.contributor.author Adhikary, Utsarga
dc.contributor.author Samaddar, Sandip
dc.contributor.author Ghosh, Chandradhish
dc.contributor.author Haldar, Jayanta
dc.date.accessioned 2017-01-04T09:09:00Z
dc.date.available 2017-01-04T09:09:00Z
dc.date.issued 2015
dc.identifier.citation Bioconjugate Chemistry en_US
dc.identifier.citation 26 en_US
dc.identifier.citation 12 en_US
dc.identifier.citation Konai, 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.identifier.issn 1043-1802
dc.identifier.uri https://libjncir.jncasr.ac.in/xmlui/10572/2009
dc.description Restricted access en_US
dc.description.abstract The 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.description.uri http://dx.doi.org/10.1021/acs.bioconjchem.5b00494 en_US
dc.language.iso English en_US
dc.publisher American Chemical Society en_US
dc.rights ?American Chemical Society, 2015 en_US
dc.subject Biochemical Research Methods en_US
dc.subject Biochemistry & Molecular Biology en_US
dc.subject Chemistry en_US
dc.subject Chemistry, Organic en_US
dc.subject Pseudomonas-Aeruginosa Biofilms en_US
dc.subject Helical Antimicrobial Peptides en_US
dc.subject Antibiotic-Resistance en_US
dc.subject Antibacterial Activity en_US
dc.subject Cationic Amphiphiles en_US
dc.subject Side-Chain en_US
dc.subject Agents en_US
dc.subject Lipopeptides en_US
dc.subject Infections en_US
dc.subject Derivatives en_US
dc.title Structure-Activity Relationship of Amino Acid Tunable Lipidated Norspermidine Conjugates: Disrupting Biofilms with Potent Activity against Bacterial Persisters en_US
dc.type Article en_US


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