Exploration of a new series of PAR1 antagonists.
Bioorg Med Chem Lett
; 20(5): 1735-9, 2010 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-20137929
ABSTRACT
Two series of new PAR1 antagonists have been identified. The first incorporates a cinnamoylpiperidine motif and the second a cinnamoylpyridine pattern. The synthesis, biological activity and structure-activity relationship of these compounds are presented. In each series, one analog showed potent in vivo antithrombotic activity in a rat AV shunt model, with up to 53% inhibition at 1.25mpk iv for compound 30.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Piridinas
/
Receptor PAR-1
/
Fibrinolíticos
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article