Tricyclic Thiazolopyrazole Derivatives as Metabotropic Glutamate Receptor 4 Positive Allosteric Modulators

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• 作者：Sang-Phyo Hong ; Kevin G. Liu ; Gil Ma ; Michael Sabio ; Michelle A. Uberti ; Maria D. Bacolod ; John Peterson ; Zack Z. Zou ; Albert J. Robichaud ; Dari虂o Doller
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：July 28, 2011
• 年：2011
• 卷：54
• 期：14
• 页码：5070-5081
• 全文大小：989K
• 年卷期：v.54,no.14(July 28, 2011)
• ISSN：1520-4804

文摘

There is an increasing amount of evidence to support that activation of the metabotropic glutamate receptor 4 (mGlu4 receptor), either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinson鈥檚 disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons. As part of our efforts in identifying therapeutics for central nervous system (CNS) diseases such as Parkinson鈥檚 disease, we have been focusing on metabotropic glutamate receptors. Herein we report our studies with a series of tricyclic thiazolopyrazoles as mGlu4 PAMs.