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VU6010608, a Novel mGlu NAM from a Series of -(2-(1-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides

Authors

Reed CW Carson W , McGowan KM Kevin M , Spearing PK Paul K , Stansley BJ Branden J , Roenfanz HF Hanna F , Engers DW Darren W , Rodriguez AL Alice L , Engelberg EM Eileen M , Luscombe VB Vincent B , Loch MT Matthew T , Remke DH Daniel H , Rook JM Jerri M , Blobaum AL Anna L , Conn PJ P Jeffrey , Niswender CM Colleen M , Lindsley CW Craig W .
ACS medicinal chemistry letters. 2017 11 8; 8(12).
1326-1330

Abstract

Herein, we report the structure-activity relationships within a series of mGlu NAMs based on an -(2-(1-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamide core with excellent CNS penetration ( 1.9-5.8 and 0.4-1.4). Analogues in this series displayed steep SAR. Of these, VU6010608 () emerged with robust efficacy in blocking high frequency stimulated long-term potentiation in electrophysiology studies.

Tags: 2017