The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2

doi:10.1016/j.bmcl.2009.11.032

Bioorganic & Medicinal Chemistry Letters

Volume 20, Issue 2, 15 January 2010, Pages 759-762

https://doi.org/10.1016/j.bmcl.2009.11.032 Get rights and content

Abstract

The optimisation of an HTS hit series (1) leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators GSK1331258 and GSK1331268 is described. Structure–activity relationships, attenuation of dopaminergic activity, and potentiation of mGluR2 responses in rat hippocampal MPP-DG synapses are also reported.

Graphical abstract

The optimisation of an HTS hit series (1) leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators GSK1331258 and GSK1331268 is described.

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The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2

Abstract

Graphical abstract

Neurosci. Lett.

Eur. J. Pharmacol.

Pharm. Theor.

Bioorg. Med. Chem. Lett.

Bioorg. Med. Chem. Lett.

Neuropharmacology

Neuropharmacology

Neuropharmacology

Neuropharmacology

J. Pharmacol. Exp. Ther.

Curr. Drug Targets CNS Neurol. Disord.

Nat. Med.

J. Pharmacol. Exp. Ther.