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代谢型谷氨酸受体4（mGluR4）新型正变构调节剂（PAM）的合成与构效关系

Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4).

作者信息

Williams Richard, Johnson Kari A, Gentry Patrick R, Niswender Colleen M, Weaver Charles D, Conn P Jeffrey, Lindsley Craig W, Hopkins Corey R

机构信息

Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.

出版信息

Bioorg Med Chem Lett. 2009 Sep 1;19(17):4967-70. doi: 10.1016/j.bmcl.2009.07.072. Epub 2009 Jul 18.

DOI:10.1016/j.bmcl.2009.07.072
PMID:19640716
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2752865/
Abstract

This Letter describes the synthesis and SAR of the novel positive allosteric modulator, VU0155041, a compound that has shown in vivo efficacy in rodent models of Parkinson's disease. The synthesis takes advantage of an iterative parallel synthesis approach to rapidly synthesize and evaluate a number of analogs of VU0155041.

摘要

本信函描述了新型正变构调节剂VU0155041的合成及构效关系，该化合物在帕金森病啮齿动物模型中已显示出体内疗效。合成过程利用迭代平行合成方法，快速合成并评估了多个VU0155041类似物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/bac4d1385baf/nihms-140686-f0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/a8fb1f114d7d/nihms-140686-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/5ca6923c66bf/nihms-140686-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/3ea07807468e/nihms-140686-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/2eda7f43cfd9/nihms-140686-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/3b006ed1554c/nihms-140686-f0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/bac4d1385baf/nihms-140686-f0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/a8fb1f114d7d/nihms-140686-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/5ca6923c66bf/nihms-140686-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/3ea07807468e/nihms-140686-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/2eda7f43cfd9/nihms-140686-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/3b006ed1554c/nihms-140686-f0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1120/2752865/bac4d1385baf/nihms-140686-f0008.jpg

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