Development of potent and selective small-molecule human Urotensin-II antagonists

This work describes the development of potent and selective human Urotensin-II antagonists starting from lead compound 1. Several problems relating to oral bioavailability, cytochrome P450 inhibition, and selectivity for hUT over other receptors were addressed. This work describes the development of...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-06, Vol.18 (12), p.3500-3503
Hauptverfasser:	McAtee, John J., Dodson, Jason W., Dowdell, Sarah E., Girard, Gerald R., Goodman, Krista B., Hilfiker, Mark A., Sehon, Clark A., Sha, Deyou, Wang, Gren Z., Wang, Ning, Viet, Andrew Q., Zhang, Daohua, Aiyar, Nambi V., Behm, David J., Carballo, Luz H., Evans, Christopher A., Fries, Harvey E., Nagilla, Rakesh, Roethke, Theresa J., Xu, Xiaoping, Yuan, Catherine C.K., Douglas, Stephen A., Neeb, Michael J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Aniline Compounds - chemical synthesis Aniline Compounds - chemistry Aniline Compounds - pharmacology Animals Antagonist Biological and medical sciences Biological Availability Cell Line Drug Evaluation, Preclinical GPR14 hU-II Humans hUT Medical sciences Molecular Structure Molecular Weight Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Piperidones - chemical synthesis Piperidones - chemistry Piperidones - pharmacology Rats Receptors, G-Protein-Coupled - antagonists & inhibitors Small Molecule Libraries Stereoisomerism Structure-Activity Relationship U-II Urotensin
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