Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: hit-to-lead optimization.
Bioorg Med Chem Lett
; 24(16): 3845-9, 2014 Aug 15.
Article
em En
| MEDLINE
| ID: mdl-25017030
ABSTRACT
An HTS campaign of our corporate compound library resulted in thieno[2,3-b]pyridines derivative hits with mGluR5 negative allosteric modulator effects. During the hit-to-lead development our objective was to improve affinity, and to keep the ligand efficiency values at an acceptable level. After different modifications of the linker resulted in a 2-sulfonyl-thieno[2,3-b]pyridines derivative, which fulfilled the lead criteria.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Tienopiridinas
/
Receptor de Glutamato Metabotrópico 5
Limite:
Humans
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article