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Bioorg Med Chem Lett. 2006 Mar 15;16(6):1527-31. Epub 2006 Jan 4.

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

Author information

1
Department of Chemistry, Hawaii Biotech Inc., 99-193 Aiea Heights Drive, Suite 200, Aiea, HI 96701, USA. gjiao@hibiotech.com

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.

PMID:
16386899
DOI:
10.1016/j.bmcl.2005.12.038
[Indexed for MEDLINE]

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