Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5

Andrew S. Felts; Sam A. Saleh; Uyen Le; Alice L. Rodriguez; C. David Weaver; P. Jeffrey Conn; Craig W. Lindsley; Kyle A. Emmitte

doi:10.1016/j.bmcl.2009.10.024

Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu₅

Andrew S. Felts, Sam A. Saleh, Uyen Le, Alice L. Rodriguez, C. David Weaver, P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte

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

17 Scopus citations

Abstract

A high-throughput cell-based screen identified a series of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of metabotropic glutamate receptor 5 (mGlu₅). This Letter describes the SAR of this series and the profile of selected compounds in selectivity and radioligand binding assays.

Original language	English
Pages (from-to)	6623-6626
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	23
DOIs	https://doi.org/10.1016/j.bmcl.2009.10.024
State	Published - 1 Dec 2009

Keywords

Glutamate
Metabotropic glutamate receptor 5
Negative allosteric modulator
Non-competitive antagonist
Quinazoline

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10.1016/j.bmcl.2009.10.024

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abstract = "A high-throughput cell-based screen identified a series of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of metabotropic glutamate receptor 5 (mGlu5). This Letter describes the SAR of this series and the profile of selected compounds in selectivity and radioligand binding assays.",

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AU - Rodriguez, Alice L.

AU - Weaver, C. David

AU - Conn, P. Jeffrey

AU - Lindsley, Craig W.

AU - Emmitte, Kyle A.

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KW - Glutamate

KW - Metabotropic glutamate receptor 5

KW - Negative allosteric modulator

KW - Non-competitive antagonist

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IS - 23

ER -

Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu₅

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Keywords

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