title: Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.
abstract: Two novel constrained l-AP4 analogues, (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines (7) and (8), were synthesized and evaluated as mGluR ligands. Compound 7 showed to be a group III mGluRs agonist with micromolar activity.
authors.affiliation: Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo, 1-06123 Perugia, Italy.
authors.forename: Laura
authors.initials: L
authors.lastname: Amori
authors.forename: Michaela
authors.initials: M
authors.lastname: Serpi
authors.forename: Maura
authors.initials: M
authors.lastname: Marinozzi
authors.forename: Gabriele
authors.initials: G
authors.lastname: Costantino
authors.forename: Monica Gavilan
authors.initials: MG
authors.lastname: Diaz
authors.forename: Mette Brunsgaard
authors.initials: MB
authors.lastname: Hermit
authors.forename: Christian
authors.initials: C
authors.lastname: Thomsen
authors.forename: Roberto
authors.initials: R
authors.lastname: Pellicciari
mesh_terms: D000818:Animals; D016466:CHO Cells; D002460:Cell Line; D006224:Cricetinae; D018698:Glutamic Acid / Q000737:chemistry; D005998:Glycine / Q000737:chemistry*; D007700:Kinetics; D008024:Ligands; D008956:Models, Chemical; D008968:Molecular Conformation; D011422:Propionates / Q000138:chemical synthesis* / Q000737:chemistry*; D011485:Protein Binding; D011487:Protein Conformation; D018094:Receptors, Metabotropic Glutamate / Q000737:chemistry*; D013237:Stereoisomerism
chemical_list: C114785:2-amino-4-phosphono-propinate; D008024:Ligands; D011422:Propionates; D018094:Receptors, Metabotropic Glutamate; D018698:Glutamic Acid; D005998:Glycine