Incorporation of Piperazino Functionality into 1,3-Disubstituted Urea as the Tertiary Pharmacophore Affording Potent Inhibitors of Soluble Epoxide Hydrolase with Improved Pharmacokinetic Properties

The inhibition of the mammalian soluble epoxide hydrolase (sEH) is a promising new therapy in the treatment of hypertension, inflammation, and other disorders. However, the problems of limited water solubility, high melting point, and low metabolic stability complicated the development of 1,3-disubs...

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Veröffentlicht in:	Journal of medicinal chemistry 2010-12, Vol.53 (23), p.8376-8386
Hauptverfasser:	Huang, Shao-Xu, Li, Hui-Yuan, Liu, Jun-Yan, Morisseau, Christophe, Hammock, Bruce D, Long, Ya-Qiu
Format:	Artikel
Sprache:	eng
Schlagworte:	Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Epoxide Hydrolases - antagonists & inhibitors Humans Inhibitory Concentration 50 Magnetic Resonance Spectroscopy Models, Molecular Piperazines - chemistry Structure-Activity Relationship Urea - chemistry
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