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

@article{Kubas2013ScaffoldHA,
  title={Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.},
  author={Holger Kubas and Udo Meyer and Mirko Hechenberger and Kai-Uwe Klein and Patrick Plitt and Ronalds Zemribo and Harm W Spexgoor and Sander G A van Assema and Ulrich Abel},
  journal={Bioorganic & medicinal chemistry letters},
  year={2013},
  volume={23 23},
  pages={6370-6}
}
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 template for a scaffold hopping approach, generating a structurally diverse set of potent analogs. Both the limited aqueous solubility and the relatively poor metabolic stability of AFQ-056 were… CONTINUE READING

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