title: Novel analogues of ketamine and phencyclidine as NMDA receptor antagonists.
abstract: The identification of structurally novel analogues of ketamine and phencyclidine (PCP), as NMDA receptor antagonists, with low to moderate potency at GluN2A and GluN2B receptors is discussed. In particular, some examples, such as compounds 6 and 10, shows decreased calculated lipophilicity, when compared to PCP, while retaining moderate activity. Moreover, the germinal aryl amino substituted lactam ring, as exemplified in compounds 7-10 and 11-13, constitutes a novel scaffold with potential application in the design of biologically active compounds.
authors.affiliation: Department of Medicinal Chemistry, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline Medicines Research Centre, via A Fleming 4, 37135 Verona, Italy. zarantonello.paola@libero.it
authors.forename: Paola
authors.initials: P
authors.lastname: Zarantonello
authors.forename: Ezio
authors.initials: E
authors.lastname: Bettini
authors.forename: Alfredo
authors.initials: A
authors.lastname: Paio
authors.forename: Chiara
authors.initials: C
authors.lastname: Simoncelli
authors.forename: Silvia
authors.initials: S
authors.lastname: Terreni
authors.forename: Francesco
authors.initials: F
authors.lastname: Cardullo
mesh_terms: D007649:Ketamine / Q000031:analogs & derivatives / Q000494:pharmacology*; D010622:Phencyclidine / Q000031:analogs & derivatives / Q000494:pharmacology*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*
chemical_list: D016194:Receptors, N-Methyl-D-Aspartate; D007649:Ketamine; D010622:Phencyclidine