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

Alice L. Rodriguez; Ya Zhou; Richard Williams; C. David Weaver; Paige N. Vinson; Eric S. Dawson; Thomas Steckler; Hilde Lavreysen; Claire MacKie; José M. Bartolomé; Gregor J. MacDonald; J. Scott Daniels; Colleen M. Niswender; Carrie K. Jones; P. Jeffrey Conn; Craig W. Lindsley; Shaun R. Stauffer

doi:10.1016/j.bmcl.2012.10.068

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

Alice L. Rodriguez
, Ya Zhou
, Richard Williams
, C. David Weaver
, Paige N. Vinson
, Eric S. Dawson
, Thomas Steckler
, Hilde Lavreysen
, Claire MacKie
, José M. Bartolomé
, Gregor J. MacDonald
, J. Scott Daniels
, Colleen M. Niswender
, Carrie K. Jones
, P. Jeffrey Conn
, Craig W. Lindsley
, Shaun R. Stauffer^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

16 Citations (Scopus)

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.

Original language	English
Pages (from-to)	7388-7392
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	22
Issue number	24
DOIs	https://doi.org/10.1016/j.bmcl.2012.10.068
Publication status	Published - 15 Dec 2012
Externally published	Yes

Bibliographical note

Funding Information:
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.

Copyright:
Copyright 2013 Elsevier B.V., All rights reserved.

Keywords

Metabotropic glutamate receptor 5 (mGlu)
Non-MPEP
Positive allosteric modulator (PAM)

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/j.bmcl.2012.10.068

Cite this

Rodriguez, A. L., Zhou, Y., Williams, R., David Weaver, C., Vinson, P. N., Dawson, E. S., Steckler, T., Lavreysen, H., MacKie, C., Bartolomé, J. M., MacDonald, G. J., Scott Daniels, J., Niswender, C. M., Jones, C. K., Jeffrey Conn, P., Lindsley, C. W., & Stauffer, S. R. (2012). Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold. Bioorganic and Medicinal Chemistry Letters, 22(24), 7388-7392. https://doi.org/10.1016/j.bmcl.2012.10.068

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

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.",

keywords = "Metabotropic glutamate receptor 5 (mGlu), Non-MPEP, Positive allosteric modulator (PAM)",

author = "Rodriguez, \{Alice L.\} and Ya Zhou and Richard Williams and \{David Weaver\}, C. and Vinson, \{Paige N.\} and Dawson, \{Eric S.\} and Thomas Steckler and Hilde Lavreysen and Claire MacKie and Bartolom{\'e}, \{Jos{\'e} M.\} and MacDonald, \{Gregor J.\} and \{Scott Daniels\}, J. and Niswender, \{Colleen M.\} and Jones, \{Carrie K.\} and \{Jeffrey Conn\}, P. and Lindsley, \{Craig W.\} and Stauffer, \{Shaun R.\}",

note = "Funding Information: 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. Copyright: Copyright 2013 Elsevier B.V., All rights reserved.",

year = "2012",

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doi = "10.1016/j.bmcl.2012.10.068",

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Rodriguez, AL, Zhou, Y, Williams, R, David Weaver, C, Vinson, PN, Dawson, ES, Steckler, T, Lavreysen, H, MacKie, C, Bartolomé, JM, MacDonald, GJ, Scott Daniels, J, Niswender, CM, Jones, CK, Jeffrey Conn, P, Lindsley, CW & Stauffer, SR 2012, 'Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold', Bioorganic and Medicinal Chemistry Letters, vol. 22, no. 24, pp. 7388-7392. https://doi.org/10.1016/j.bmcl.2012.10.068

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AU - Rodriguez, Alice L.

AU - Zhou, Ya

AU - Williams, Richard

AU - David Weaver, C.

AU - Vinson, Paige N.

AU - Dawson, Eric S.

AU - Steckler, Thomas

AU - Lavreysen, Hilde

AU - MacKie, Claire

AU - Bartolomé, José M.

AU - MacDonald, Gregor J.

AU - Scott Daniels, J.

AU - Niswender, Colleen M.

AU - Jones, Carrie K.

AU - Jeffrey Conn, P.

AU - Lindsley, Craig W.

AU - Stauffer, Shaun R.

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PY - 2012/12/15

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