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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:22

Article

Rodriguez, Alice L.^1,2  Zhou, Ya^1,2,3  Williams, Richard^1,2  Weaver, C. David^1,5  Vinson, Paige N.^1,2,3  Dawson, Eric S.^1,2,3  Steckler, Thomas⁶  Lavreysen, Hilde⁶  Mackie, Claire⁷  Bartolome, Jose M.⁶  Macdonald, Gregor J.⁶  Daniels, J. Scott^1,2,3  Niswender, Colleen M.^1,2,3  Jones, Carrie K.^1,2,3  Conn, P. Jeffrey^1,2,3  Lindsley, Craig W.^1,2,3,4  Stauffer, Shaun R.^1,2,3,4 

[1] Vanderbilt Univ, Med Ctr, Dept Pharmacol, Nashville, TN 37232 USA

[2] Vanderbilt Univ, Med Ctr, Vanderbilt Ctr Neurosci Drug Discovery, Nashville, TN 37232 USA

[3] Vanderbilt Specialized Chem Ctr Probe Dev MLPCN, Nashville, TN 37232 USA

[4] Vanderbilt Univ, Dept Chem, Nashville, TN 37232 USA

[5] Vanderbilt Univ, Vanderbilt Inst Chem Biol, Nashville, TN 37232 USA

[6] Janssen Res & Dev, Neurosci, Beerse, Belgium

[7] Janssen Res & Dev, CREATe ADME Tox, Beerse, Belgium

关键词: Metabotropic glutamate receptor 5 (mGlu(5));    Positive allosteric modulator (PAM);    Non-MPEP;   

DOI  :  10.1016/j.bmcl.2012.10.068

来源: Elsevier

【 摘 要 】

Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on an aryl glycine sulfonamide scaffold. This series represents a rare non-MPEP site mGlu(5) PAM chemotype. (C) 2012 Elsevier Ltd. All rights reserved.

【 授权许可】

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