Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.
Bioorg Med Chem Lett
; 21(12): 3813-7, 2011 Jun 15.
Article
em En
| MEDLINE
| ID: mdl-21596563
ABSTRACT
Synthesis and structure-activity relationships (SAR) of a novel series of vasopressin V(1b) antagonists are described. 2-(6-Aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide have been identified with low nanomolar affinity for the V(1b) receptor and good selectivity with respect to related receptors V(1a), V(2) and OT. Optimised compound 16 shows a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quinazolinonas
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Antagonistas dos Receptores de Hormônios Antidiuréticos
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Sistema Hipotálamo-Hipofisário
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Acetamidas
Limite:
Animals
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Humans
/
Male
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article