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  • Title: Synthesis and antibacterial activity of novel water-soluble nocathiacin analogs.
    Author: Xu L, Farthing AK, Dropinski JF, Meinke PT, McCallum C, Hickey E, Liu K.
    Journal: Bioorg Med Chem Lett; 2013 Jan 01; 23(1):366-9. PubMed ID: 23164707.
    Abstract:
    Semi-synthetic water-soluble analogs were synthesized from nocathiacin I through the formation of a versatile intermediate nocathiacin amine 5, and subsequent transformation via reductive amination, acylation or urea formation. Several of the novel analogs displayed much improved aqueous solubility over 1, while retained antibacterial activity. Compound 15 and 16 from the amide series, demonstrated excellent in vitro and in vivo antibacterial activity.
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