Glycolipids and benzylammonium lipids as novel antisepsis agents: synthesis and biological characterization.

Abstract

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.

• Authors: Matteo Piazza, Clara Rossini, Silvia Della Fiorentina, Chiara Pozzi, Francesca Comelli, Isabella Bettoni, Paola Fusi, Barbara Costa, Francesco Peri
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 52 Issue 4 Pg. 1209-13 (Feb 26 2009) ISSN: 1520-4804 [Electronic] United States
• PMID: 19161283 (Publication Type: Journal Article)

Chemical References

• Anti-Infective Agents
• Benzylammonium Compounds
• Glycolipids
• Lipid A
• Lipids

Topics

• Anti-Infective Agents (chemical synthesis, pharmacology)
• Benzylammonium Compounds (chemical synthesis, pharmacology)
• Cell Line
• Drug Design
• Glycolipids (chemical synthesis, pharmacology)
• Humans
• Lipid A (antagonists & inhibitors)
• Lipids (chemical synthesis, pharmacology)
• Sepsis (drug therapy)
• Shock, Septic (drug therapy)
• Structure-Activity Relationship