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  • Title: 1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.
    Author: 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.
    Journal: J Med Chem; 2003 Mar 13; 46(6):913-6. PubMed ID: 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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