2. Academic Validation
  3. 1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo

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. doi: 10.1021/jm0255926.
Alan C Tinker 1,  Haydn G Beaton,  Nigel Boughton-Smith,  Tony R Cook,  Sally L Cooper,  Lynne Fraser-Rae,  Kay Hallam,  Peter Hamley,  Tom McInally,  David J Nicholls,  Austen D Pimm,  Alan V Wallace
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, AstraZeneca R & D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK. [email protected]
PMID: 12620067 DOI: 10.1021/jm0255926
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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