Issue 2, 2011

New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2). Identification and synthesis of N-propyl-5-substituted isoquinolones

Abstract

A series of N-propyl-5-substituted isoquinolones was identified as positive allosteric modulators (PAM) of metabotropic glutamate receptor 2 (mGluR2) via high-throughput screening (HTS). The subsequent synthesis and preliminary SAR exploration that led to the identification of compound 20 are described.

Graphical abstract: New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2). Identification and synthesis of N-propyl-5-substituted isoquinolones

Article information

Article type
Concise Article
Submitted
03 Nov 2010
Accepted
30 Nov 2010
First published
17 Dec 2010

Med. Chem. Commun., 2011,2, 132-139

New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2). Identification and synthesis of N-propyl-5-substituted isoquinolones

A. A. Trabanco, G. Duvey, J. M. Cid, G. J. Macdonald, P. Cluzeau, V. Nhem, R. Furnari, N. Behaj, G. Poulain, T. Finn, S. Poli, H. Lavreysen, A. Raux, Y. Thollon, N. Poirier, D. D'Addona, J. I. Andrés, R. Lutjens, E. Le Poul, H. Imogai and J. Rocher, Med. Chem. Commun., 2011, 2, 132 DOI: 10.1039/C0MD00200C

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