5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.
Bioorg Med Chem Lett
; 8(21): 2955-60, 1998 Nov 03.
Article
em En
| MEDLINE
| ID: mdl-9873654
ABSTRACT
Synthesis of a variety of 5,5-trans fused lactones, related to compounds found in extracts of Lantana camara, has provided a series of novel acylating inhibitors of human thrombin, trypsin, chymotrypsin and human leucocyte elastase. The most effective thrombin inhibitor is 7 with an IC50 of 130 nM and a Kobs/[1] of 4,000 M-1 s-1.
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Base de dados:
MEDLINE
Assunto principal:
Trombina
/
Inibidores de Serina Proteinase
/
Lactonas
Tipo de estudo:
Diagnostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
1998
Tipo de documento:
Article