3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency.
3-Phenyl-3.4-dihydro-1-isoquinolinamine is a weak inhibitor of iNOS and nNOS. Structural variation of 5a results in inhibitors with a range of potency and selectivity for the NOS enzymes, including a potent and very selective iNOS inhibitor 5j.
Beaton
H
H
Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Loughborough, UK.
Hamley
P
P
Nicholls
D J
DJ
Tinker
A C
AC
Wallace
A V
AV
D000818:Animals; D002478:Cells, Cultured; D002531:Cerebellum / Q000166:cytology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D007546:Isoquinolines / Q000737:chemistry / Q000494:pharmacology*; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors*; D052248:Nitric Oxide Synthase Type I; D052247:Nitric Oxide Synthase Type II; D020033:Protein Isoforms / Q000037:antagonists & inhibitors; D051381:Rats; D012680:Sensitivity and Specificity
D004791:Enzyme Inhibitors; D007546:Isoquinolines; D020033:Protein Isoforms; C496320:NOS1 protein, human; C496319:NOS2 protein, human; D019001:Nitric Oxide Synthase; D052248:Nitric Oxide Synthase Type I; D052247:Nitric Oxide Synthase Type II; C496322:Nos1 protein, rat; C496318:Nos2 protein, rat