Optimization of a Tertiary Alcohol Series of Phosphodiesterase-4 (PDE4) Inhibitors: Structure−Activity Relationship Related to PDE4 Inhibition and Human Ether-a-go-go Related Gene Potassium Channel Binding Affinity

A SAR study on the tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors related to 1 is described. In addition to inhibitory potency against PDE4 and the lipopolysaccharide-induced production of TNFα in human whole blood, the binding affinity of these compounds for the human ether-a-go-g...

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Veröffentlicht in:	Journal of medicinal chemistry 2003-06, Vol.46 (12), p.2413-2426
Hauptverfasser:	Friesen, Richard W, Ducharme, Yves, Ball, Richard G, Blouin, Marc, Boulet, Louise, Côté, Bernard, Frenette, Richard, Girard, Mario, Guay, Daniel, Huang, Zheng, Jones, Thomas R, Laliberté, France, Lynch, Joseph J, Mancini, Joseph, Martins, Evelyn, Masson, Paul, Muise, Eric, Pon, Douglas J, Siegl, Peter K. S, Styhler, Angela, Tsou, Nancy N, Turner, Mervyn J, Young, Robert N, Girard, Yves
Format:	Artikel
Sprache:	eng
Schlagworte:	3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors Alcohols - chemical synthesis Alcohols - pharmacokinetics Alcohols - pharmacology Alcohols - toxicity Animals Biological and medical sciences Bronchoconstriction - drug effects Cardiovascular system Crystallography, X-Ray Cyclic N-Oxides - chemical synthesis Cyclic N-Oxides - pharmacokinetics Cyclic N-Oxides - pharmacology Cyclic N-Oxides - toxicity Cyclic Nucleotide Phosphodiesterases, Type 4 Dogs Electrocardiography ERG1 Potassium Channel Ether-A-Go-Go Potassium Channels Guinea Pigs Humans In Vitro Techniques Long QT Syndrome - chemically induced Medical sciences Miscellaneous Pharmacology. Drug treatments Phosphodiesterase Inhibitors - chemical synthesis Phosphodiesterase Inhibitors - pharmacokinetics Phosphodiesterase Inhibitors - pharmacology Phosphodiesterase Inhibitors - toxicity Potassium Channels - metabolism Potassium Channels, Voltage-Gated Protein Binding Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacokinetics Pyridines - pharmacology Pyridines - toxicity Rats Respiratory system Saimiri Sheep Stereoisomerism Structure-Activity Relationship Tumor Necrosis Factor-alpha - biosynthesis Vomiting - chemically induced
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