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Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.
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- Additional Information
- Source:
Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print Cited Medium: Print ISSN: 0022-2623 (Print) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
- Publication Information:
Publication: Washington Dc : American Chemical Society
Original Publication: [Easton, Pa.] : American Chemical Society, [c1963-
- Subject Terms:
- Abstract:
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 (pIC(50) = 8.6-9.4). The N-cycloheptyl- and N-adamantanyltetrahydrophthalazinones (7h, 8, 10, 11) show high in vivo antiinflammatory activities after oral application. Additionally, some phthalazinones were found to exhibit potent suppression of LPS-induced TNFalpha release and show moderate potency against fMLP-stimulated production of ROS.
- Accession Number:
0 (Anti-Inflammatory Agents, Non-Steroidal)
0 (Cycloheptanes)
0 (Enzyme Inhibitors)
0 (Lipopolysaccharides)
0 (Phthalazines)
0 (Reactive Oxygen Species)
0 (Tumor Necrosis Factor-alpha)
EC 3.1.4.17 (3',5'-Cyclic-AMP Phosphodiesterases)
EC 3.1.4.17 (Cyclic Nucleotide Phosphodiesterases, Type 3)
EC 3.1.4.17 (Cyclic Nucleotide Phosphodiesterases, Type 4)
PJY633525U (Adamantane)
- Publication Date:
Date Created: 20020531 Date Completed: 20020627 Latest Revision: 20190710
- Publication Date:
20231215
- Accession Number:
10.1021/jm0110340
- Accession Number:
12036360
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