Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu(5)

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

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(23): 6623-6626.

DOI：10.1016/j.bmcl.2009.10.024

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

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

• 出版日期2009-12-1