VU6010608, a Novel mGlu NAM from a Series of -(2-(1-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides
AUTHORS
Reed
CWCarson W ,
McGowan
KMKevin M ,
Spearing
PKPaul K ,
Stansley
BJBranden J ,
Roenfanz
HFHanna F ,
Engers
DWDarren W ,
Rodriguez
ALAlice L ,
Engelberg
EMEileen M ,
Luscombe
VBVincent B ,
Loch
MTMatthew T ,
Remke
DHDaniel H ,
Rook
JMJerri M ,
Blobaum
ALAnna L ,
Conn
PJP Jeffrey ,
Niswender
CMColleen M ,
Lindsley
CWCraig W .
ACS medicinal chemistry letters. 2017 11 8; 8(12).
1326-1330
- PMID: 29259756[PubMed].
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