Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.
Bioorg Med Chem Lett
; 13(5): 795-8, 2003 Mar 10.
Article
em En
| MEDLINE
| ID: mdl-12617893
ABSTRACT
Starting from a 2-amino-6-methylpyridine P1 group and following a strategy of enlarging it whilst reducing its polarity, we have developed a series of potent, moderately basic azaindoles which are intrinsically much more selective for thrombin versus trypsin. Certain pyrazinone acetamide azaindole derivatives have pharmacokinetic parameters after oral administration to dogs, or efficacy in vitro, comparable to an optimized pyrazinone acetamide 2-amino-6-methylpyridine derivative.
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Base de dados:
MEDLINE
Assunto principal:
Compostos Aza
/
Trombina
/
Inibidores Enzimáticos
/
Indóis
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2003
Tipo de documento:
Article