VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides,ACS Medicinal Chemistry Letters

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VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-11-10 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00429
Carson W. Reed , Kevin M. McGowan , Paul K. Spearing , Branden J. Stansley , Hanna F. Roenfanz , Darren W. Engers , Alice L. Rodriguez , Eileen M. Engelberg , Vincent B. Luscombe , Matthew T. Loch , Daniel H. Remke , Jerri M. Rook , Anna L. Blobaum , P. Jeffrey Conn ₁ , Colleen M. Niswender ₁ , Craig W. Lindsley

Affiliation

Herein, we report the structure–activity relationships within a series of mGlu₇ NAMs based on an N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamide core with excellent CNS penetration (K_p 1.9–5.8 and K_p,uu 0.4–1.4). Analogues in this series displayed steep SAR. Of these, VU6010608 (11a) emerged with robust efficacy in blocking high frequency stimulated long-term potentiation in electrophysiology studies.

中文翻译：

VU6010608，来自一系列N-（2-（1 H -1,2,4-三唑-1-基）-5-（三氟甲氧基）苯基）苯甲酰胺的新型mGlu ₇ NAM

在这里，我们报告一系列基于N-（2-（1 H -1,2,4-三唑-1-基）-5-（三氟甲氧基）苯基）苯甲酰胺核心的mGlu ₇ NAM中的结构活性关系具有出色的CNS渗透性（K _p 1.9-5.8和K _p，uu 0.4-1.4）。该系列中的类似物显示出陡峭的SAR。其中，VU6010608（11a）在阻断电生理研究中的高频刺激的长期增强作用方面表现出强大的功效。

更新日期：2017-11-10

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