Design, synthesis and preliminary evaluation of novel 3 '-substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors

Authors
Pellicciari, R Costantino, G Marinozzi, M Macchiarulo, A Amori, L Flor, PJ Gasparini, F Kuhn, R Urwyler, S
Citation
R. Pellicciari et al., Design, synthesis and preliminary evaluation of novel 3 '-substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors, BIOORG MED, 11(24), 2001, pp. 3179-3182
Citations number
25
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
24
Year of publication
2001
Pages
3179 - 3182
Database
ISI
SICI code
0960-894X(200112)11:24<3179:DSAPEO>2.0.ZU;2-L
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 ant agonist with submicromolar activity. (C) 2001 Elsevier Science Ltd. All rig hts reserved.