Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists
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DOI：
10.1016/j.bmcl.2006.12.033
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发表时间：
2007-03-01
影响因子：
2.7
通讯作者：
Spooren, Will
中科院分区：
文献类型：
--
作者：
Jaeschke, Georg;Porter, Richard;Spooren, Will
亲和力和微粒体稳定性的优化导致鉴定出有效的代谢稳定的非诺班类似物41。在四种不同的焦虑模型中证明了41的稳健体内功效。此外，提出了一种基于配体的药效团对齐的非诺班和MPEP。(c)2007爱思唯尔有限公司保留所有权利。
Optimization of affinity and microsomal stability led to identification of the potent, metabolically stable fenobam analog 41. Robust in vivo efficacy of 41 was demonstrated in four different models of anxiety. Additionally, a ligand based pharmacophore alignment of fenobant and MPEP is proposed. (c) 2007 Elsevier Ltd. All rights reserved.