Macrocyclic factor XIa inhibitors.
Bioorg Med Chem Lett
; 27(17): 4056-4060, 2017 09 01.
Article
em En
| MEDLINE
| ID: mdl-28780160
ABSTRACT
A series of macrocyclic factor XIa (FXIa) inhibitors was designed based on an analysis of the crystal structures of the acyclic phenylimidazole compounds. Further optimization using structure-based design led to inhibitors with pM affinity for FXIa, excellent selectivity against a panel of relevant serine proteases, and good potency in the activated partial thromboplastin time (aPTT) clotting assay.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Fator XIa
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Inibidores de Serina Proteinase
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Compostos Macrocíclicos
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Imidazóis
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article