title: Design, synthesis and preliminary evaluation of novel 3'-substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors.
abstract: Two novel 3'-substituted carboxycylopropylglycines, (2S,1'S,2'S,3'R)-2-(3'-xanthenylmethyl-2'-carboxycyclopropyl)glycine (8a) and (2S,1'S,2'S,3'R)-2-(3'-xanthenylethyl-2'-carboxycyclopropyl)glycine (8b), were synthesized and evaluated as mGluR ligands. Compound 8b showed to be a potent group II antagonist with submicromolar activity.
authors.affiliation: Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo 1, 06127, Perugia, Italy. rp@unipg.it
authors.forename: R
authors.initials: R
authors.lastname: Pellicciari
authors.forename: G
authors.initials: G
authors.lastname: Costantino
authors.forename: M
authors.initials: M
authors.lastname: Marinozzi
authors.forename: A
authors.initials: A
authors.lastname: Macchiarulo
authors.forename: L
authors.initials: L
authors.lastname: Amori
authors.forename: P
authors.initials: P
authors.lastname: Josef Flor
authors.forename: F
authors.initials: F
authors.lastname: Gasparini
authors.forename: R
authors.initials: R
authors.lastname: Kuhn
authors.forename: S
authors.initials: S
authors.lastname: Urwyler
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D004353:Drug Evaluation, Preclinical; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D005998:Glycine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*
chemical_list: D018691:Excitatory Amino Acid Antagonists; D018094:Receptors, Metabotropic Glutamate; D005998:Glycine