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

Andrés A. Trabanco; Guillaume Duvey; José María Cid; Gregor J. Macdonald; Philippe Cluzeau; Vanthea Nhem; Rocco Furnari; Nadia Behaj; Géraldine Poulain; Terry Finn; Sonia Poli; Hilde Lavreysen; Alexandre Raux; Yves Thollon; Nicolas Poirier; David D'Addona; José Ignacio Andrés; Robert Lutjens; Emmanuel Le Poul; Hassan Imogai; Jean-Philippe Rocher

doi:10.1039/C0MD00200C

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

Andrés A. Trabanco,*^a Guillaume Duvey,^b José María Cid,^a Gregor J. Macdonald,^c Philippe Cluzeau,^b Vanthea Nhem,^b Rocco Furnari,^b Nadia Behaj,^b Géraldine Poulain,^b Terry Finn,^b Sonia Poli,^b Hilde Lavreysen,^d Alexandre Raux,^b Yves Thollon,^b Nicolas Poirier,^b David D'Addona,^b José Ignacio Andrés,^a Robert Lutjens,^b Emmanuel Le Poul,^b Hassan Imogai^b and Jean-Philippe Rocher^b

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* Corresponding authors

^a Medicinal Chemistry, Janssen Research & Development, Janssen-Cilag S.A., Polígono Industrial, Calle Jarama 75, Toledo, Spain
E-mail: atrabanc@its.jnj.com

^b Addex Pharmaceuticals, 12 chemin des Aulx, Plan-les-Ouates, Geneva, Switzerland

^c Medicinal Chemistry, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse, Belgium

^d Neuroscience, Janssen Research & Development, Janssen Pharmaceutica N.V., Turnhoutseweg 30, Beerse, Belgium

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.

MedChemComm

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

Abstract

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

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