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 anti-sepsis drug development. In addition in the studies presented in this PhD thesis new classes of natural compounds are tested for their ability to interact with TLR4 receptor complex.
(2009). Synthesis and biological characterization of novel TLR4 ligands. (Tesi di dottorato, Università degli Studi di Milano-Bicocca, 2009).
Synthesis and biological characterization of novel TLR4 ligands
PIAZZA, MATTEO
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 anti-sepsis drug development. In addition in the studies presented in this PhD thesis new classes of natural compounds are tested for their ability to interact with TLR4 receptor complex.
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phd_unimib_035230.pdf
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Doctoral thesis
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