Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters










Database
Language
Publication year range
1.
Bioorg Med Chem Lett ; 23(23): 6370-6, 2013 Dec 01.
Article in English | MEDLINE | ID: mdl-24125886

ABSTRACT

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.


Subject(s)
Indoles/chemistry , Indoles/pharmacology , Receptor, Metabotropic Glutamate 5/metabolism , Allosteric Regulation , Animals , CHO Cells , Cricetulus , Crystallography, X-Ray , Humans , Models, Molecular , Receptor, Metabotropic Glutamate 5/chemistry , Structure-Activity Relationship
SELECTION OF CITATIONS
SEARCH DETAIL
...