Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.
Bioorg Med Chem Lett
; 11(2): 243-6, 2001 Jan 22.
Article
em En
| MEDLINE
| ID: mdl-11206469
ABSTRACT
Described are the acylation binding of trans-lactam 1 to porcine pancreatic elastase, the selection of the SO2Me activating group for the lactam N which also confers metabolic stability in hamster liver microsomes, the introduction of aqueous solubility through the piperidine salt 9, the in vivo oral activity of 9 and its bioavailability, and the introduction of 9 as an intracellular neutrophil elastase inhibitor.
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Base de dados:
MEDLINE
Assunto principal:
Elastase de Leucócito
/
Lactamas
/
Neutrófilos
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2001
Tipo de documento:
Article