The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
Bioorg Med Chem Lett
; 12(18): 2603-6, 2002 Sep 16.
Article
em En
| MEDLINE
| ID: mdl-12182870
ABSTRACT
The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency and very encouraging developability properties. Diethylaminoethyl derivative 32, SB-435495, was selected for progression to man.
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Base de dados:
MEDLINE
Assunto principal:
Fosfolipases A
/
Pirimidinonas
/
Compostos de Bifenilo
/
Inibidores Enzimáticos
/
Lipoproteínas
Idioma:
En
Ano de publicação:
2002
Tipo de documento:
Article