| Autor: |
Tinker AC; Department of Medicinal Chemistry, AstraZeneca R & D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK. Alan.C.Tinker@Astrazeneca.com, Beaton HG, Boughton-Smith N, Cook TR, Cooper SL, Fraser-Rae L, Hallam K, Hamley P, McInally T, Nicholls DJ, Pimm AD, Wallace AV |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2003 Mar 13; Vol. 46 (6), pp. 913-6. |
| DOI: |
10.1021/jm0255926 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
