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


AUTHORS

Rodriguez ALAlice L , Zhou Y Ya , Williams R Richard , Weaver CD C David , Vinson PN Paige N , Dawson ES Eric S , Steckler T Thomas , Lavreysen H Hilde , Mackie C Claire , Bartolomé JM José M , Macdonald GJ Gregor J , Daniels JS J Scott , Niswender CM Colleen M , Jones CK Carrie K , Conn PJ P Jeffrey , Lindsley CW Craig W , Stauffer SR Shaun R . Bioorganic & medicinal chemistry letters. 2012 12 15; 22(24). 7388-92

ABSTRACT

Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on an aryl glycine sulfonamide scaffold. This series represents a rare non-MPEP site mGlu(5) PAM chemotype.


Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on an aryl glycine sulfonamide scaffold. This series represents a rare non-MPEP site mGlu(5) PAM chemotype.