Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

Chad E. Bennett; Duane A. Burnett; William J. Greenlee; Chad E. Knutson; Peter Korakas; Cheng Li; Deen Tulshian; Wen Lian Wu; Rosalia Bertorelli; Silva Fredduzzi; Mariagrazia Grilli; Gianluca Lozza; Angelo Reggiani; Alessio Veltri

doi:10.1016/j.bmcl.2011.12.131

Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

Chad E. Bennett
, Duane A. Burnett
, William J. Greenlee
, Chad E. Knutson
, Peter Korakas
, Cheng Li
, Deen Tulshian
, Wen Lian Wu
, Rosalia Bertorelli
, Silva Fredduzzi
, Mariagrazia Grilli
, Gianluca Lozza
, Angelo Reggiani
, Alessio Veltri

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

Abstract

A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGluR5. When dosed orally, several examples were active in vivo in a rat SNL test.

Original language	English
Pages (from-to)	1575-1578
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	22
Issue number	4
DOIs	https://doi.org/10.1016/j.bmcl.2011.12.131
Publication status	Published - 15 Feb 2012
Externally published	Yes

Keywords

Fused tricyclic pyridones
GPCR
MGluR1 (metabotropic glutamate receptor 1)
Neuropathic pain
Spinal nerve ligation (SNL)

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10.1016/j.bmcl.2011.12.131

Cite this

Bennett, C. E., Burnett, D. A., Greenlee, W. J., Knutson, C. E., Korakas, P., Li, C., Tulshian, D., Wu, W. L., Bertorelli, R., Fredduzzi, S., Grilli, M., Lozza, G., Reggiani, A., & Veltri, A. (2012). Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain. Bioorganic and Medicinal Chemistry Letters, 22(4), 1575-1578. https://doi.org/10.1016/j.bmcl.2011.12.131

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doi = "10.1016/j.bmcl.2011.12.131",

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AU - Bennett, Chad E.

AU - Burnett, Duane A.

AU - Greenlee, William J.

AU - Knutson, Chad E.

AU - Korakas, Peter

AU - Li, Cheng

AU - Tulshian, Deen

AU - Wu, Wen Lian

AU - Bertorelli, Rosalia

AU - Fredduzzi, Silva

AU - Grilli, Mariagrazia

AU - Lozza, Gianluca

AU - Reggiani, Angelo

AU - Veltri, Alessio

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AB - A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGluR5. When dosed orally, several examples were active in vivo in a rat SNL test.

KW - Fused tricyclic pyridones

KW - GPCR

KW - MGluR1 (metabotropic glutamate receptor 1)

KW - Neuropathic pain

KW - Spinal nerve ligation (SNL)

UR - https://www.scopus.com/pages/publications/84862826031

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DO - 10.1016/j.bmcl.2011.12.131

M3 - Article

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VL - 22

SP - 1575

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 4

ER -

Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

Abstract

Keywords

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