1.
Bioorg Med Chem Lett
; 20(12): 3737-41, 2010 Jun 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20483612
RESUMO
Here we report the discovery and early SAR of a series of mGluR5 negative allosteric modulators (NAMs). Starting from a moderately active HTS hit we synthesized 3,5-disubstituted-oxadiazoles and tetrazoles as mGluR5 NAMs. Based on the analysis of ligand efficiency and lipophilic efficiency metrics we identified a promising lead candidate as a starting point for further optimization.