化学
代谢型谷氨酸受体
代谢型谷氨酸受体5
代谢型谷氨酸受体1
谷氨酸受体
代谢型谷氨酸受体2
脚手架
代谢型谷氨酸受体3
药理学
代谢型谷氨酸受体7
变构调节
代谢型谷氨酸受体6
变构调节剂
组合化学
生物物理学
神经科学
受体
生物化学
生物
计算机科学
数据库
作者
Holger Kubas,Udo Meyer,Mirko Hechenberger,Kai-Uwe Klein,Patrick Plitt,Ronalds Zemribo,Harm W. Spexgoor,Sander G. A. van Assema,Ulrich Abel
标识
DOI:10.1016/j.bmcl.2013.09.059
摘要
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 improved with hexahydrocyclopenta[c]pyrrole derivative 54a, which proved to be a valuable candidate for further development.
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