Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles.
Bioorg Med Chem Lett
; 11(4): 509-13, 2001 Feb 26.
Article
em En
| MEDLINE
| ID: mdl-11229759
ABSTRACT
A nonpeptidyl GnRH receptor antagonist (1), with a unique 2-arylindole core, was identified through the Merck in-house screening for binding affinity on the rat GnRH receptor. SAR studies directed toward the alkoxy-ethanolamine and 2-aryl groups resulted in a simpler lead structure with improved activity. This compound 50 exhibits a 60-fold improvement in binding activity over our initial lead 1.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores LHRH
/
Indóis
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2001
Tipo de documento:
Article
País de afiliação:
Estados Unidos