Design and synthesis of potent and selective macrocyclic thrombin inhibitors.
Bioorg Med Chem Lett
; 13(16): 2781-4, 2003 Aug 18.
Article
en En
| MEDLINE
| ID: mdl-12873514
ABSTRACT
A series of potent and selective proline- and pyrazinone-based macrocyclic thrombin inhibitors is described. Detailed SAR studies led to the incorporation of specific functional groups in the tether that enhanced functional activity against thrombin and provided exquisite selectivity against trypsin and tPA. X-ray crystallography and molecular modeling studies revealed the inhibitor-enzyme interactions responsible for this selectivity.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Antitrombinas
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2003
Tipo del documento:
Article
País de afiliación:
Estados Unidos