Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold

doi:10.1016/j.bmcl.2012.10.068

Bioorganic & Medicinal Chemistry Letters

Volume 22, Issue 24, 15 December 2012, Pages 7388-7392

https://doi.org/10.1016/j.bmcl.2012.10.068 Get rights and content

Abstract

Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulators (PAMs) based on an aryl glycine sulfonamide scaffold. This series represents a rare non-MPEP site mGlu₅ PAM chemotype.

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Acknowledgments

This work was supported in part by grants from the NIH (NS031373, MH062646, and MH89870) and from an industry sponsored contract from Johnson & Johnson. Vanderbilt is a member of the MLPCN and houses the Vanderbilt Specialized Chemistry Center for Accelerated Probe Development (U54MH084659). The authors thank Daryl F. Venable and Kiran K. Gogi for technical assistance.

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Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold

Abstract

Graphical abstract

Section snippets

Acknowledgments

Trends Pharm. Sci.

Neuropharmacology

Bioorg. Med. Chem. Lett.

Bioorg. Med. Chem. Lett.

Bioorg. Med. Chem. Lett.

Bioorg. Med. Chem. Lett.

Curr. Topics Med. Chem.

Curr. Opin. Drug Disc. Dev.

Nat. Rev. Drug Disc.

Curr. Topics Med. Chem.

Nature

Mol. Pharmacol.

J. Med. Chem.

Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold