新型代谢型谷氨酸受体 2（mGluR2）别构调节剂的发现和合成：N-丙基-8-氯-6-取代异喹啉酮的研究。
New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones.
机构信息
Medicinal Chemistry, Janssen Research & Development, Janssen-Cilag SA, Toledo, Spain.
出版信息
Bioorg Med Chem Lett. 2011 Feb 1;21(3):971-6. doi: 10.1016/j.bmcl.2010.12.048. Epub 2010 Dec 21.
PMID:21232953
Abstract
A series of N-propyl-8-chloro-6-substituted isoquinolones was identified as positive allosteric modulators of metabotropic glutamate receptor 2 (mGluR2 PAM) via high throughput screening (HTS). The subsequent synthesis and initial SAR exploration that led to the identification of compound 28 is described.
摘要
通过高通量筛选（HTS），一系列 N-丙基-8-氯-6-取代异喹啉酮被鉴定为代谢型谷氨酸受体 2（mGluR2 PAM）的正别构调节剂。随后的合成和初步 SAR 探索导致了化合物 28 的鉴定，本文对此进行了描述。
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