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

Bioorganic & Medicinal Chemistry Letters
2001.0

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.

Knowledge Graph

Similar Paper

Design, synthesis and preliminary evaluation of novel 3′-Substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors
Bioorganic & Medicinal Chemistry Letters 2001.0
(2S,1‘S,2‘R,3‘R)-2-(2‘-Carboxy-3‘-hydroxymethylcyclopropyl) Glycine Is a Highly Potent Group 2 and 3 Metabotropic Glutamate Receptor Agonist with Oral Activity
Journal of Medicinal Chemistry 2004.0
(2S,1‘S,2‘S,3‘R)-2-(2‘-Carboxy-3‘-methylcyclopropyl) Glycine Is a Potent and Selective Metabotropic Group 2 Receptor Agonist with Anxiolytic Properties
Journal of Medicinal Chemistry 2002.0
A highly selective agonist for the metabotropic glutamate receptor mGluR2
MedChemComm 2011.0
(2S,1′S,2′R,3′R)-2(2′-Carboxy-3′-hydroxymethylcyclopropyl)glycine-[3H], a potent and selective radioligand for labeling group 2 and 3 metabotropic glutamate receptors
Bioorganic & Medicinal Chemistry Letters 2005.0
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
Bioorganic & Medicinal Chemistry Letters 2006.0
Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III
Bioorganic & Medicinal Chemistry Letters 2000.0
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2′-phosphono-3′-phenylcyclopropyl)glycine, the first class of 3′-substituted transC1′−2′-2-(2′-phosphonocyclopropyl)glycines
Bioorganic & Medicinal Chemistry 2007.0
Development of 2′-Substituted (2S,1′R,2′S)-2-(Carboxycyclopropyl)glycine Analogues as Potent N-Methyl-<scp>d</scp>-aspartic Acid Receptor Agonists
Journal of Medicinal Chemistry 2013.0
New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III
Journal of Medicinal Chemistry 2016.0