4-Aminopyrimidine tetrahydronaphthols: A series of novel vanilloid receptor-1 antagonists with improved solubility properties

8-(6-(4-(Trifluoromethyl)phenyl)pyrimidin-4-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol ( 4) and analogs ( 5– 10) were shown to be potent inhibitors of human and rat TRPV1 in vitro with increased solubility over our previous series. Synthesis, SAR, and improvements in metabolic stability and absorpti...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-03, Vol.18 (6), p.1830-1834
Hauptverfasser:	Doherty, Elizabeth M., Retz, Daniel, Gavva, Narender R., Tamir, Rami, Treanor, James J.S., Norman, Mark H.
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics Animals Benzothiazoles - pharmacology Biological and medical sciences Blood Flow Velocity - drug effects Calcium - metabolism Capsaicin - pharmacology CHO Cells Chromatography, High Pressure Liquid Cricetinae Cricetulus Hepatocytes - cytology Hepatocytes - drug effects Hepatocytes - metabolism Humans Medical sciences Metabolic Clearance Rate Molecular Structure Naphthols - chemical synthesis Naphthols - pharmacokinetics Naphthols - pharmacology Neuropharmacology Pharmacology. Drug treatments Pyrimidines - chemical synthesis Pyrimidines - pharmacokinetics Pyrimidines - pharmacology Rats Solubility Structure-Activity Relationship TRPV Cation Channels - antagonists & inhibitors TRPV1 VR1
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Zusammenfassung:	8-(6-(4-(Trifluoromethyl)phenyl)pyrimidin-4-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol ( 4) and analogs ( 5– 10) were shown to be potent inhibitors of human and rat TRPV1 in vitro with increased solubility over our previous series. Synthesis, SAR, and improvements in metabolic stability and absorption of these compounds are described herein.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.02.022