Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.
Bioorg Med Chem Lett
; 15(3): 527-30, 2005 Feb 01.
Article
en En
| MEDLINE
| ID: mdl-15664806
ABSTRACT
A series of novel ortho-substituted cinnamic acids have been synthesized, and their binding activity and selectivity on the four prostaglandin E(2) receptors evaluated. Many of them are very potent and selective EP(3) antagonists (K(i) 3-10 nM), while compound 9 is a very good and selective EP(2) agonist (K(i) 8 nM). The biological profile of the EP(2) agonist 9 in vivo and the metabolic profile of selected EP(3) antagonists are also reported.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Cinamatos
/
Receptores de Prostaglandina E
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2005
Tipo del documento:
Article