Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives

The optimization of a cyclopentane-based hNK1 antagonist scaffold will be discussed in the context of enhanced water-solubility, sub-nanomolar hNK1 binding affinity, and oral activity in two in vivo models. The synthesis and optimization of a cyclopentane-based hNK1 antagonist scaffold 3, having fou...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-09, Vol.16 (17), p.4504-4511
Hauptverfasser:	Meurer, Laura C., Finke, Paul E., Owens, Karen A., Tsou, Nancy N., Ball, Richard G., Mills, Sander G., MacCoss, Malcolm, Sadowski, Sharon, Cascieri, Margaret A., Tsao, Kwei-Lan, Chicchi, Gary G., Egger, Linda A., Luell, Silvi, Metzger, Joseph M., MacIntyre, D. Euan, Rupniak, Nadia M.J., Williams, Angela R., Hargreaves, Richard J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Biological and medical sciences CHO Cells Cricetinae Cyclopentanes - adverse effects Cyclopentanes - chemical synthesis Cyclopentanes - chemistry Cyclopentanes - pharmacology Humans Medical sciences Molecular Structure Neurokinin-1 Receptor Antagonists Neurokinin-1: substance P Neuropharmacology Neurotransmitters. Neurotransmission. Receptors NK1 antagonist: cyclopentane-based structure Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Receptors, Neurokinin-1 - genetics Receptors, Neurokinin-1 - metabolism Solubility Structure-Activity Relationship Water
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