Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors.
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.
Jaroch
Stefan
S
Department of Medicinal Chemistry, Research Center Europe, Corporate Research, Schering AG, D-13342-, Berlin, Germany. stefan.jaroch@shering.de
Hölscher
Peter
P
Rehwinkel
Hartmut
H
Sülzle
Detlev
D
Burton
Gerardine
G
Hillmann
Margrit
M
McDonald
Fiona M
FM
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
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