Title of article
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
Author/Authors
Laura Amori، نويسنده , , Gabriele Costantino، نويسنده , , Maura Marinozzi، نويسنده , , Roberto Pellicciari، نويسنده , , Fabrizio Gasparini، نويسنده , , Peter J. Flor، نويسنده , , Rainer Kuhn، نويسنده , , Ivo Vranesic، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
4
From page
1447
To page
1450
Abstract
On the basis of a pharmacophore definition of mGlu4 agonists, the two novel semi-rigid derivatives 12 and 13 were designed and synthesized. The preliminary biological evaluation demonstrated that both compounds interact with hmGlu4a, while ineffective at group II receptor subtypes. In particular, derivative 13 is a full hmGlu4a agonist with an EC50=17 μM.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790893
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