Novel Selective PDE4 Inhibitors. 3. In Vivo Antiinflammatory Activity of a New Series of N-Substituted cis-Tetra- and cis-Hexahydrophthalazinones

The synthesis and biological activities of a series of N-substituted cis-4a,5,6,7,8,8a-hexa- and cis-4a,5,8,8a-tetrahydro-2H-phthalazin-1-ones are described. It was found that compounds bearing a cycloalkyl group at the 2-position exhibit the highest PDE4 inhibitory activities (pIC50 = 8.6−9.4). The...

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Veröffentlicht in:	Journal of medicinal chemistry 2002-06, Vol.45 (12), p.2520-2525
Hauptverfasser:	Van der Mey, Margaretha, Boss, Hildegard, Hatzelmann, Armin, Van der Laan, Ivonne J, Sterk, Geert J, Timmerman, Hendrik
Format:	Artikel
Sprache:	eng
Schlagworte:	3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors Adamantane - analogs & derivatives Adamantane - chemical synthesis Adamantane - chemistry Adamantane - pharmacology Administration, Oral Animals Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacology Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cyclic Nucleotide Phosphodiesterases, Type 3 Cyclic Nucleotide Phosphodiesterases, Type 4 Cycloheptanes - chemical synthesis Cycloheptanes - chemistry Cycloheptanes - pharmacology Edema - drug therapy Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Female Humans In Vitro Techniques Leukocytes, Mononuclear - drug effects Leukocytes, Mononuclear - metabolism Lipopolysaccharides - pharmacology Luminescent Measurements Medical sciences Mice Pharmacology. Drug treatments Phthalazines - chemical synthesis Phthalazines - chemistry Phthalazines - pharmacology Reactive Oxygen Species - metabolism Structure-Activity Relationship Tumor Necrosis Factor-alpha - metabolism
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