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ID: ALA1146910

Journal: Bioorg Med Chem Lett

Title: Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease.

Authors: Jiao GS, Simo O, Nagata M, O'Malley S, Hemscheidt T, Cregar L, Millis SZ, Goldman ME, Tang C.

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.

CiteXplore: 16870442

DOI: 10.1016/j.bmcl.2006.07.005