Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators

The metabotropic glutamate receptor subtype 5 has evolved into a promising target for the treatment of various diseases of the central nervous system, such as Fragile X and l-DOPA induced dyskinesia. One of the most advanced clinical compound is Novartis’ AFQ-056 (Mavoglurant), which served us as a...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-12, Vol.23 (23), p.6370-6376
Hauptverfasser:	Kubas, Holger, Meyer, Udo, Hechenberger, Mirko, Klein, Kai-Uwe, Plitt, Patrick, Zemribo, Ronalds, Spexgoor, Harm W., van Assema, Sander G.A., Abel, Ulrich
Format:	Artikel
Sprache:	eng
Schlagworte:	AFQ-056 Allosteric modulator Allosteric properties Allosteric Regulation Animals CHO Cells Cricetulus Crystallography, X-Ray dyskinesia glutamic acid Humans Indoles - chemistry Indoles - pharmacology L-dopa Metabotropic glutamate receptor mGluR5 Models, Molecular Receptor, Metabotropic Glutamate 5 - chemistry Receptor, Metabotropic Glutamate 5 - metabolism Scaffold hopping solubility Structure-Activity Relationship
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