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

Authors
Amori, L Costantino, G Marinozzi, M Pellicciari, R Gasparini, F Flor, PJ Kuhn, R Vranesic, I
Citation
L. Amori et al., 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, BIOORG MED, 10(13), 2000, pp. 1447-1450
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
13
Year of publication
2000
Pages
1447 - 1450
Database
ISI
SICI code
0960-894X(20000703)10:13<1447:SMMAPB>2.0.ZU;2-A
Abstract
On the basis of a pharmacophore definition of mGlu(4) agonists, the two nov el semi-rigid derivatives 12 and 13 were designed and synthesized. The prel iminary biological evaluation demonstrated that both compounds interact wit h hmGlu(4a), while ineffective at group II receptor subtypes. In particular . derivative 13 is a full hmGlu(4a) agonist with an EC50= 17 mu M. (C) 2000 Elsevier Science Ltd. All rights reserved.