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.
| Original language | English |
|---|---|
| Pages (from-to) | 1209-1213 |
| Number of pages | 5 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 52 |
| Issue number | 4 |
| DOIs | |
| Publication status | Published - Feb 26 2009 |
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ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery
Cite this
Glycolipids and benzylammonium lipids as novel antisepsis agents : Synthesis and biological characterization. / Piazza, Matteo; Rossini, Clara; Fiorentina, Silvia Delia; Pozzi, Chiara; Comelli, Francesca; Bettoni, Isabella; Fusi, Paola; Costa, Barbara; Peri, Francesco.
In: Journal of Medicinal Chemistry, Vol. 52, No. 4, 26.02.2009, p. 1209-1213.Research output: Contribution to journal › Article
}
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.
UR - http://www.scopus.com/inward/record.url?scp=64349098670&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=64349098670&partnerID=8YFLogxK
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 -