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

R Pellicciari; G Costantino; M Marinozzi; A Macchiarulo; L Amori; P Josef Flor; F Gasparini; R Kuhn; S Urwyler

doi:10.1016/s0960-894x(01)00656-4

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

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3179-82. doi: 10.1016/s0960-894x(01)00656-4.

Authors

R Pellicciari¹, G Costantino, M Marinozzi, A Macchiarulo, L Amori, P Josef Flor, F Gasparini, R Kuhn, S Urwyler

Affiliation

¹ Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo 1, 06127, Perugia, Italy. rp@unipg.it

PMID: 11720869
DOI: 10.1016/s0960-894x(01)00656-4

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