Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease
摘要:
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. (c) 2006 Elsevier Ltd. All rights reserved.
N-(tert-Butoxycarbonyloxy)-5-norbornene-endo-2,3-dicarboximide, a Reagent for the Regioselective Introduction of the tert-Butoxycarbonyl (BOC) Protective Group at Unhindered Amines: Application to Amino glycoside Chemistry
Novel conjugates of polysaccharides and uses thereof
申请人:Lapidot Aviva
公开号:US20060166867A1
公开(公告)日:2006-07-27
Novel conjugates composed of a saccharide-containing moiety (e.g., aminoglycosides) covalently linked to a moiety containing two or more basic amino acid residues (e.g., a polyarginine) and processes of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing these conjugates and uses of these conjugates as antiviral and antibacterial agents.