1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.
Article Details
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Tinker AC, Beaton HG, Boughton-Smith N, Cook TR, Cooper SL, Fraser-Rae L, Hallam K, Hamley P, McInally T, Nicholls DJ, Pimm AD, Wallace AV
1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.
J Med Chem. 2003 Mar 13;46(6):913-6.
- PubMed ID
- 12620067 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 1-(6-CYANO-3-PYRIDYLCARBONYL)-5',8'-DIFLUOROSPIRO[PIPERIDINE-4,2'(1'H)-QUINAZOLINE]-4'-AMINE Nitric oxide synthase, inducible IC 50 (nM) 37 N/A N/A Details Pimagedine Nitric oxide synthase, inducible IC 50 (nM) 3900 N/A N/A Details