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  • Title: Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease.
    Author: Jiao GS, Simo O, Nagata M, O'Malley S, Hemscheidt T, Cregar L, Millis SZ, Goldman ME, Tang C.
    Journal: Bioorg Med Chem Lett; 2006 Oct 01; 16(19):5183-9. PubMed ID: 16870442.
    Abstract:
    A series of mono-, di-, and tri-guanidinylated derivatives of neamine were prepared via selective guanidinylation of neamine. These molecules represent a novel scaffold as inhibitors of anthrax lethal factor zinc metalloprotease. Methods for the synthesis of these compounds are described, and structure-activity relationships among the series are analyzed. In addition, initial findings regarding the mechanism of LF inhibition for these molecules are presented.
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