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.
MeSH terms
-
Animals
-
CHO Cells
-
Cricetinae
-
Drug Evaluation, Preclinical
-
Excitatory Amino Acid Antagonists / chemical synthesis*
-
Excitatory Amino Acid Antagonists / pharmacology*
-
Glycine / analogs & derivatives
-
Glycine / chemical synthesis*
-
Glycine / pharmacology*
-
Receptors, Metabotropic Glutamate / antagonists & inhibitors*
Substances
-
Excitatory Amino Acid Antagonists
-
Receptors, Metabotropic Glutamate
-
Glycine