title: Glycolipids and benzylammonium lipids as novel antisepsis agents: synthesis and biological characterization.
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.
authors.affiliation: Department of Biotechnology and Biosciences, University of Milano-Bicocca, Piazza della Scienza 2, 20126 Milano, Italy.
authors.forename: Matteo
authors.initials: M
authors.lastname: Piazza
authors.forename: Clara
authors.initials: C
authors.lastname: Rossini
authors.forename: Silvia
authors.initials: S
authors.lastname: Della Fiorentina
authors.forename: Chiara
authors.initials: C
authors.lastname: Pozzi
authors.forename: Francesca
authors.initials: F
authors.lastname: Comelli
authors.forename: Isabella
authors.initials: I
authors.lastname: Bettoni
authors.forename: Paola
authors.initials: P
authors.lastname: Fusi
authors.forename: Barbara
authors.initials: B
authors.lastname: Costa
authors.forename: Francesco
authors.initials: F
authors.lastname: Peri
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D050339:Benzylammonium Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D015195:Drug Design; D006017:Glycolipids / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D008050:Lipid A / Q000037:antagonists & inhibitors; D008055:Lipids / Q000138:chemical synthesis* / Q000494:pharmacology; D018805:Sepsis / Q000188:drug therapy*; D012772:Shock, Septic / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D050339:Benzylammonium Compounds; D006017:Glycolipids; D008050:Lipid A; D008055:Lipids