Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain.
Bioorg Med Chem Lett
; 22(23): 7223-6, 2012 Dec 01.
Article
en En
| MEDLINE
| ID: mdl-23084894
ABSTRACT
High throughput screening identified the pyridothienopyrimidinone 1 as a ligand for the metabotropic glutamate receptor 1 (mGluR1=10 nM). Compound 1 has an excellent in vivo profile; however, it displays unfavorable pharmacokinetic issues and metabolic stability. Therefore, using 1 as a template, novel analogues (10i) were prepared. These analogues displayed improved oral exposure and activity in the Spinal Nerve Ligation (SNL) pain model.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Pirimidinonas
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Tiofenos
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Receptores de Glutamato Metabotrópico
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Compuestos Heterocíclicos con 3 Anillos
Límite:
Animals
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Humans
Idioma:
En
Año:
2012
Tipo del documento:
Article