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


AUTHORS

Felts ASAndrew S , Saleh SA Sam A , Le U Uyen , Rodriguez AL Alice L , Weaver CD C David , Conn PJ P Jeffrey , Lindsley CW Craig W , Emmitte KA Kyle A . Bioorganic & medicinal chemistry letters. 2009 12 1; 19(23). 6623-6

ABSTRACT

A high-throughput cell-based screen identified a series of 6-substituted-4-anilinoquinazolines as non-competitive 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.


A high-throughput cell-based screen identified a series of 6-substituted-4-anilinoquinazolines as non-competitive 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.