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.
Piazza, M., Rossini, C., Della Fiorentina, S., Pozzi, C., Comelli, F., Bettoni, I., et al. (2009). Glycolipids and Benzylammonium Lipids as Novel Antisepsis Agents: Synthesis and Biological Characterization. JOURNAL OF MEDICINAL CHEMISTRY, 52(4), 1209-1213 [10.1021/jm801333m].
Glycolipids and benzylammonium lipids as novel antisepsis agents: Synthesis and biological characterization
PIAZZA, MATTEO;POZZI, CHIARA;COMELLI, FRANCESCA;BETTONI, ISABELLA;FUSI, PAOLA ALESSANDRA;COSTA, BARBARA SIMONA;PERI, FRANCESCO
2009
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.
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