Discovery of heteroaryl sulfonamides as new EP1 receptor selective antagonists.
Bioorg Med Chem
; 14(19): 6628-39, 2006 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-16784865
ABSTRACT
4-({2-[Isobutyl(phenylsulfonyl)amino]-5-(trifluoromethyl)phenoxy}methyl)benzoic acid (1) is a functional PGE2 antagonist selective for EP1 receptor subtype. Analogs of 1, in which the phenyl-sulfonyl moiety has been replaced with more hydrophilic heteroarylsulfonyl moieties, exhibited more optimized antagonist activity, while some of them showed in vivo antagonist activity. Structure-activity relationship (SAR) studies are also presented.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sulfonamidas
/
Alprostadil
/
Receptores de Prostaglandina E
Limite:
Animals
/
Female
/
Humans
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article