Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.
Bioorg Med Chem Lett
; 13(2): 161-4, 2003 Jan 20.
Article
em En
| MEDLINE
| ID: mdl-12482415
ABSTRACT
Use of a chlorophenoxyacetamide P1 group with a pyridinone acetamide P2/P3 gave an exceptionally potent thrombin inhibitor (K(i)=40 pM). Truncation of the molecule at the N-terminus gave unique, low nanomolar, non-covalent thrombin inhibitors which do not have a group to fill thrombin's 'distal binding pocket'. A co-crystal structure indicates the importance of an intramolecular hydrogen bond between the P1 side chain and P1/P2 amide link in this series.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piridonas
/
Trombina
/
Inibidores Enzimáticos
/
Acetamidas
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2003
Tipo de documento:
Article