Potent, Highly Selective, and Orally Bioavailable Gem-Difluorinated Monocationic Inhibitors of Neuronal Nitric Oxide Synthase

In our efforts to discover neuronal isoform selective nitric oxide synthase (NOS) inhibitors, we have developed a series of compounds containing a pyrrolidine ring with two stereogenic centers. The enantiomerically pure compounds, (S,S) versus (R,R), exhibited two different binding orientations, wit...

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Veröffentlicht in:	Journal of the American Chemical Society 2010-10, Vol.132 (40), p.14229-14238
Hauptverfasser:	Xue, Fengtian, Li, Huiying, Delker, Silvia L, Fang, Jianguo, Martásek, Pavel, Roman, Linda J, Poulos, Thomas L, Silverman, Richard B
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Biological Availability Catalytic Domain Crystallography, X-Ray Enzyme Inhibitors - administration & dosage Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Models, Molecular Molecular Structure Nitric Oxide Synthase Type I - antagonists & inhibitors Rats
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