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.
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.
Amori
Laura
L
Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo, 1-06123 Perugia, Italy.
Serpi
Michaela
M
Marinozzi
Maura
M
Costantino
Gabriele
G
Diaz
Monica Gavilan
MG
Hermit
Mette Brunsgaard
MB
Thomsen
Christian
C
Pellicciari
Roberto
R
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
C114785:2-amino-4-phosphono-propinate; D008024:Ligands; D011422:Propionates; D018094:Receptors, Metabotropic Glutamate; D018698:Glutamic Acid; D005998:Glycine