Guanidinylated 2,5-dideoxystreptamine Derivatives As Anthrax Lethal Factor Inhibitors

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2006 Jan 3

PMID 16386899

Citations 10

Authors

Guan-Sheng Jiao

Lynne Cregar

Mark E Goldman

Sherri Z Millis

Cho Tang

Affiliations

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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.

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