Document Report Card

ID: ALA1136724

Journal: J Med Chem

Title: 1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.

Authors: 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.

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.

CiteXplore: 12620067

DOI: 10.1021/jm0255926