PMID- 12620067
OWN - NLM
STAT- MEDLINE
DCOM- 20030407
LR  - 20051117
IS  - 0022-2623 (Print)
IS  - 0022-2623 (Linking)
VI  - 46
IP  - 6
DP  - 2003 Mar 13
TI  - 1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible 
      nitric oxide synthase which show antiinflammatory activity in vivo.
PG  - 913-6
AB  - 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.
FAU - Tinker, Alan C
AU  - Tinker AC
AD  - Department of Medicinal Chemistry, AstraZeneca R & D Charnwood, Bakewell Road, 
      Loughborough, Leicestershire LE11 5RH, UK. Alan.C.Tinker@Astrazeneca.com
FAU - Beaton, Haydn G
AU  - Beaton HG
FAU - Boughton-Smith, Nigel
AU  - Boughton-Smith N
FAU - Cook, Tony R
AU  - Cook TR
FAU - Cooper, Sally L
AU  - Cooper SL
FAU - Fraser-Rae, Lynne
AU  - Fraser-Rae L
FAU - Hallam, Kay
AU  - Hallam K
FAU - Hamley, Peter
AU  - Hamley P
FAU - McInally, Tom
AU  - McInally T
FAU - Nicholls, David J
AU  - Nicholls DJ
FAU - Pimm, Austen D
AU  - Pimm AD
FAU - Wallace, Alan V
AU  - Wallace AV
LA  - eng
PT  - Journal Article
PL  - United States
TA  - J Med Chem
JT  - Journal of medicinal chemistry
JID - 9716531
RN  - 0 (Amines)
RN  - 0 (Enzyme Inhibitors)
RN  - 0 (Isoenzymes)
RN  - 0 (Quinazolines)
RN  - 0 (Spiro Compounds)
RN  - EC 1.14.13.39 (Nitric Oxide Synthase)
RN  - EC 1.14.13.39 (Nitric Oxide Synthase Type II)
RN  - EC 1.14.13.39 (Nos2 protein, rat)
SB  - IM
MH  - Acute Disease
MH  - Administration, Oral
MH  - Amines/chemical synthesis/chemistry/pharmacology
MH  - Animals
MH  - Arthritis, Experimental/drug therapy
MH  - Cell Line
MH  - Chronic Disease
MH  - Enzyme Inhibitors/*chemical synthesis/chemistry/pharmacology
MH  - Injections, Intravenous
MH  - Isoenzymes/antagonists & inhibitors
MH  - Nitric Oxide Synthase/*antagonists & inhibitors
MH  - Nitric Oxide Synthase Type II
MH  - Quinazolines/*chemical synthesis/chemistry/pharmacology
MH  - Rats
MH  - Spiro Compounds/chemical synthesis/chemistry/pharmacology
MH  - Structure-Activity Relationship
EDAT- 2003/03/07 04:00
MHDA- 2003/04/08 05:00
CRDT- 2003/03/07 04:00
PHST- 2003/03/07 04:00 [pubmed]
PHST- 2003/04/08 05:00 [medline]
PHST- 2003/03/07 04:00 [entrez]
AID - 10.1021/jm0255926 [doi]
PST - ppublish
SO  - J Med Chem. 2003 Mar 13;46(6):913-6. doi: 10.1021/jm0255926.