TY - JOUR
T1 - Glycolipids and benzylammonium lipids as novel antisepsis agents
T2 - Synthesis and biological characterization
AU - Piazza, Matteo
AU - Rossini, Clara
AU - Fiorentina, Silvia Delia
AU - Pozzi, Chiara
AU - Comelli, Francesca
AU - Bettoni, Isabella
AU - Fusi, Paola
AU - Costa, Barbara
AU - Peri, Francesco
PY - 2009/2/26
Y1 - 2009/2/26
N2 - 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.
AB - 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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U2 - 10.1021/jm801333m
DO - 10.1021/jm801333m
M3 - Article
C2 - 19161283
AN - SCOPUS:64349098670
VL - 52
SP - 1209
EP - 1213
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 4
ER -