Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs.
Bioorg Med Chem Lett
; 20(12): 3737-41, 2010 Jun 15.
Article
em En
| MEDLINE
| ID: mdl-20483612
ABSTRACT
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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Oxidiazóis
/
Tetrazóis
/
Receptores de Glutamato Metabotrópico
/
Regulação Alostérica
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2010
Tipo de documento:
Article
País de afiliação:
Hungria