[摘要]:New glycolipids and a benzylammonium lipid were rationally designed by varying the chem. structure of a D-glucose-derived hit compd. active as lipid A antagonist. The synthesis of these compds. is reported, and their in vitro activity as lipid A antagonists on HEK cells and the capacity to inhibit LPS-induced septic shock in vivo are also discussed. The lack of toxicity and the good in vivo activity suggest the use of some compds. of the panel as hits for antisepsis drug development.