کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1367498 981635 2006 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Novel endotoxin-sequestering compounds with terephthalaldehyde-bis-guanylhydrazone scaffolds
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Novel endotoxin-sequestering compounds with terephthalaldehyde-bis-guanylhydrazone scaffolds
چکیده انگلیسی

We have shown that lipopolyamines bind to the lipid A moiety of lipopolysaccharide, a constituent of Gram-negative bacterial membranes, and neutralize its toxicity in animal models of endotoxic shock. In an effort to identify non-polyamine scaffolds with similar endotoxin-recognizing features, we had observed an unusually high frequency of hits containing guanylhydrazone scaffolds in high-throughput screens. We now describe the syntheses and preliminary structure–activity relationships in a homologous series of bis-guanylhydrazone compounds decorated with hydrophobic functionalities. These first-generation compounds bind and neutralize lipopolysaccharide with a potency comparable to that of polymyxin B, a peptide antibiotic known to sequester LPS.

A homologous series of bis-guanylhydrazone compounds decorated with hydrophobic functionalities bind and neutralize lipopolysaccharide (LPS) with a potency comparable to that of polymyxin B, a peptide antibiotic known to sequester LPS.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 5, 1 March 2006, Pages 1305–1308
نویسندگان
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