Glycolipids and Benzylammonium Lipids as Novel Antisepsis Agents: Synthesis and Biological Characterization

详细信息    查看全文

• 作者：Matteo Piazza ; Clara Rossini ; Silvia Della Fiorentina ; Chiara Pozzi ; Francesca Comelli ; Isabella Bettoni ; Paola Fusi ; Barbara Costa ; Francesco Peri*
• 刊名：Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：February 26, 2009
• 年：2009
• 卷：52
• 期：4
• 页码：1209-1213
• 全文大小：136K
• 年卷期：v.52,no.4(February 26, 2009)
• ISSN：1520-4804

文摘

New glycolipids and a benzylammonium lipid were rationally designed by varying the chemical structure of a d-glucose-derived hit compound active as lipid A antagonist. We report the synthesis of these compounds, their in vitro activity as lipid A antagonists on HEK cells, and the capacity to inhibit LPS-induced septic shock in vivo. The lack of toxicity and the good in vivo activity suggest the use of some compounds of the panel as hits for antisepsis drug development.