1. Glycolipids and benzylammonium lipids as novel antisepsis agents: synthesis and biological characterization.
- Author
-
Piazza M, Rossini C, Della Fiorentina S, Pozzi C, Comelli F, Bettoni I, Fusi P, Costa B, and Peri F
- Subjects
- Anti-Infective Agents pharmacology, Benzylammonium Compounds pharmacology, Cell Line, Drug Design, Glycolipids pharmacology, Humans, Lipid A antagonists & inhibitors, Lipids pharmacology, Shock, Septic drug therapy, Structure-Activity Relationship, Anti-Infective Agents chemical synthesis, Benzylammonium Compounds chemical synthesis, Glycolipids chemical synthesis, Lipids chemical synthesis, Sepsis drug therapy
- 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.
- Published
- 2009
- Full Text
- View/download PDF