Design and synthesis of conformationally restricted eight-Membered ring diketones as potential serine protease inhibitors.
Bioorg Med Chem Lett
; 12(17): 2359-62, 2002 Sep 02.
Article
em En
| MEDLINE
| ID: mdl-12161133
ABSTRACT
The design of conformationally restricted eight-membered ring diketones as transition state mimics of the mechanism of action of cyclotheonamides on serine proteases is described. Two target compounds are prepared from mutilin, derived from the natural product pleuromutilin. Compound 3 shows significant inhibition of plasmin and urokinase in enzyme rate assays, but an analogue 4 in which the amide moiety has been omitted does not. An X-ray crystal structure of the diketone 3 confirms the conformational predictions made by molecular modelling.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Inibidores de Serina Proteinase
/
Cetonas
Tipo de estudo:
Prognostic_studies
Idioma:
En
Ano de publicação:
2002
Tipo de documento:
Article