1,4-Cyclohexanecarboxylates: Potent and Selective Inhibitors of Phosophodiesterase 4 for the Treatment of Asthma

Evaluation of a variety of PDE4 inhibitors in a series of cellular and in vivo assays suggested a strategy to improve the therapeutic index of PDE4 inhibitors by increasing their selectivity for the ability to inhibit PDE4 catalytic activity versus the ability to compete for high affinity [3H]rolipr...

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Veröffentlicht in:	Journal of medicinal chemistry 1998-03, Vol.41 (6), p.821-835
Hauptverfasser:	Christensen, Siegfried B, Guider, Aimee, Forster, Cornelia J, Gleason, John G, Bender, Paul E, Karpinski, Joseph M, DeWolf, Walter E, Barnette, Mary S, Underwood, David C, Griswold, Don E, Cieslinski, Lenora B, Burman, Miriam, Bochnowicz, Steven, Osborn, Ruth R, Manning, Carol D, Grous, Marilyn, Hillegas, Leonard M, Bartus, Joan O'Leary, Ryan, M. Dominic, Eggleston, Drake S, Haltiwanger, R. Curtis, Torphy, Theodore J
Format:	Artikel
Sprache:	eng
Schlagworte:	3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors Animals Anti-Asthmatic Agents - chemical synthesis Anti-Asthmatic Agents - metabolism Anti-Asthmatic Agents - pharmacology Anti-Asthmatic Agents - toxicity Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - metabolism Anti-Inflammatory Agents, Non-Steroidal - pharmacology Anti-Inflammatory Agents, Non-Steroidal - toxicity Binding, Competitive Biological and medical sciences Body Temperature - drug effects Brain - metabolism Bronchoconstriction - drug effects Cyclic Nucleotide Phosphodiesterases, Type 4 Cyclohexanecarboxylic Acids - chemical synthesis Cyclohexanecarboxylic Acids - metabolism Cyclohexanecarboxylic Acids - pharmacology Cyclohexanecarboxylic Acids - toxicity Dogs Gastric Acid - secretion Guinea Pigs Humans Medical sciences Mice Monocytes - drug effects Monocytes - metabolism Nitriles Pharmacology. Drug treatments Phosphodiesterase Inhibitors - chemical synthesis Phosphodiesterase Inhibitors - metabolism Phosphodiesterase Inhibitors - pharmacology Phosphodiesterase Inhibitors - toxicity Pyrrolidinones - chemical synthesis Pyrrolidinones - metabolism Pyrrolidinones - pharmacology Pyrrolidinones - toxicity Rabbits Recombinant Proteins - antagonists & inhibitors Respiratory system Rolipram Stereoisomerism Structure-Activity Relationship Tumor Necrosis Factor-alpha - antagonists & inhibitors Vomiting - chemically induced
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