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    Structural Correlates of Antibacterial and Membrane-Permeabilizing Activities in Acylpolyamines

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    DavidS_DuttaA_AAC_50(3)852.pdf (258.8Kb)
    Issue Date
    2006-03
    Author
    Balakrishna, Rajalakshmi
    Wood, Stewart J.
    Nguyen, Thuan B.
    Miller, Kelly A.
    Kumar, E. V. K. Suresh
    Datta, Apurba
    David, Sunil A.
    Publisher
    The American Society for Microbiology
    Type
    Article
    Article Version
    Scholarly/refereed, publisher version
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    Abstract
    A homologous series of mono- and bis-acyl polyamines with varying acyl chain lengths originally synthesized for the purpose of sequestering lipopolysaccharide were evaluated for antimicrobial activity to test the hypothesis that these bis-cationic amphipathic compounds may also bind to and permeabilize intact gram-negative bacterial membranes. Some compounds were found to possess significant antimicrobial activity, mediated via permeabilization of bacterial membranes. Structure-activity relationship studies revealed a strong dependence of the acyl chain length on antimicrobial potency and permeabilization activity. Homologated spermine, bis-acylated with C8 or C9 chains, was found to profoundly sensitize Escherichia coli to hydrophobic antibiotics such as rifampin. Nonspecific cytotoxicity is a potential drawback of these membranophilic compounds. However, the surface activity of these cationic amphipaths is strongly attenuated under physiological conditions via binding to serum albumin. Significant antibacterial activity is still retained in the presence of physiological concentrations of human serum albumin, suggesting that these compounds may serve as leads in the development of novel adjuncts to conventional antimicrobial chemotherapy.
    URI
    http://hdl.handle.net/1808/17654
    DOI
    https://doi.org/10.1128/AAC.50.3.852-861.2006
    Collections
    • Medicinal Chemistry Scholarly Works [255]
    Citation
    Balakrishna et. al. "Structural Correlates of Antibacterial and Membrane-Permeabilizing Activities in Acylpolyamines." Antimicrob. Agents Chemother. March 2006 vol. 50 no. 3 852-861 . http://dx.doi.org/10.1128/AAC.50.3.852-861.2006

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    Contact KU ScholarWorks
    785-864-8983
    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    Image Credits
     

     

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