4,5-Disubstituted-1,3-oxazolidin-2-imine derivatives: a new class of orally bioavailable nitric oxide synthase inhibitor.
In our search for a novel class of inducible nitric oxide synthase (iNOS) inhibitors, 1,3-oxazolidin-2-imine was found to weakly inhibit iNOS. Further modifications of this compound resulted in a remarkable increase in both the in vivo and in vitro inhibitory activity and selectivity for iNOS.
Ueda
Shigeo
S
Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd, Enoki-cho 33-94, Suita, 564-0053, Osaka, Japan. shigeo-ueda@dainippon-pharm.co.jp
Terauchi
Hideo
H
Yano
Akihiro
A
Ido
Motoharu
M
Matsumoto
Masashi
M
Kawasaki
Motoji
M
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D006574:Heterocyclic Compounds, 2-Ring / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D051379:Mice; D008810:Mice, Inbred C57BL; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D023303:Oxazolidinones / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology
D004791:Enzyme Inhibitors; D006574:Heterocyclic Compounds, 2-Ring; D023303:Oxazolidinones; D019001:Nitric Oxide Synthase