1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.
J Med Chem
; 46(6): 913-6, 2003 Mar 13.
Article
em En
| MEDLINE
| ID: mdl-12620067
ABSTRACT
The discovery of a novel class of nitric oxide synthase (NOS) inhibitors, 2-substituted 1,2-dihydro-4-quinazolinamines, and the related 4'-aminospiro[piperidine-4,2'(1'H)-quinazolin]-4'-amines is described. Members of both series exhibit nanomolar potency and high selectivity for the inducible isoform of the enzyme (i-NOS) relative to the constitutive isoforms in vitro. Efficacy in acute and chronic animal models of inflammatory disease following oral administration has also been demonstrated using these compounds.
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Base de dados:
MEDLINE
Assunto principal:
Quinazolinas
/
Óxido Nítrico Sintase
/
Inibidores Enzimáticos
Limite:
Animals
Idioma:
En
Ano de publicação:
2003
Tipo de documento:
Article