title: Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors.
abstract: Dihydroquinolines with aminoalkyl side chains have been synthesized and have been shown to be potent n-NOS inhibitors. A marked selectivity versus e-NOS of up to approximately 300-fold was observed, whereas i-NOS was moderately inhibited.
authors.affiliation: Department of Medicinal Chemistry, Research Center Europe, Corporate Research, Schering AG, D-13342-, Berlin, Germany. stefan.jaroch@shering.de
authors.forename: Stefan
authors.initials: S
authors.lastname: Jaroch
authors.forename: Peter
authors.initials: P
authors.lastname: Hölscher
authors.forename: Hartmut
authors.initials: H
authors.lastname: Rehwinkel
authors.forename: Detlev
authors.initials: D
authors.lastname: Sülzle
authors.forename: Gerardine
authors.initials: G
authors.lastname: Burton
authors.forename: Margrit
authors.initials: M
authors.lastname: Hillmann
authors.forename: Fiona M
authors.initials: FM
authors.lastname: McDonald
mesh_terms: D000588:Amines / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors*; D052248:Nitric Oxide Synthase Type I; D052247:Nitric Oxide Synthase Type II; D052250:Nitric Oxide Synthase Type III; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D012016:Reference Values; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D004791:Enzyme Inhibitors; D011804:Quinolines; D011994:Recombinant Proteins; C496320:NOS1 protein, human; C496319:NOS2 protein, human; C496314:NOS3 protein, human; D019001:Nitric Oxide Synthase; D052248:Nitric Oxide Synthase Type I; D052247:Nitric Oxide Synthase Type II; D052250:Nitric Oxide Synthase Type III