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ID: ALA1146060

Journal: Bioorg Med Chem Lett

Title: Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors.

Authors: Jiao GS, Cregar L, Goldman ME, Millis SZ, Tang C.

Abstract: Anthrax lethal factor is a Zn(2+)-dependent metalloprotease and the key virulence factor of tripartite anthrax toxin secreted by Bacillus anthracis, the causative agent of anthrax. A series of guanidinylated 2,5-dideoxystreptamine derivatives were designed and synthesized as inhibitors of lethal factor, some of which show strong inhibitory activity against lethal factor in an in vitro FRET assay. Preparation and structure-activity relationships of these compounds are presented.

CiteXplore: 16386899

DOI: 10.1016/j.bmcl.2005.12.038