Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.

Van der Mey M; Boss H; Hatzelmann A; Van der Laan IJ; Sterk GJ; Timmerman H

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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.

机译：新型选择性PDE4抑制剂。 3.一系列新的N-取代的顺-四-和顺-六氢邻苯二氮酮的体内抗炎活性。

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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.

机译：描述了一系列N-取代的顺式4a，5,6,7,8,8a-六-和顺式4a，5,8,8a-四氢-2H-酞嗪-1-酮的合成和生物学活性。发现在2-位带有环烷基的化合物表现出最高的PDE4抑制活性（pIC（50）= 8.6-9.4）。 N-环庚基-和N-金刚烷基四氢邻苯二氮酮（7h，8、10、11）在口服后显示出很高的体内抗炎活性。另外，发现一些邻苯二氮酮显示出对LPS诱导的TNFα释放的有效抑制作用，并且对fMLP刺激的ROS产生适度的作用。

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《Journal of Medicinal Chemistry》 |2002年第12期|共6页
作者
Van der Mey M; Boss H; Hatzelmann A; Van der Laan IJ; Sterk GJ; Timmerman H;
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正文语种 eng
中图分类药学;
关键词
Upper Case En; 4a; inhibitors; in vivo; Psychological suppression;

机译：大写字母En;4a;抑制剂;体内;心理抑制;

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1. Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones. [J] . Van der Mey M, Boss H, Hatzelmann A, Journal of Medicinal Chemistry . 2002,第12期

机译：新型选择性PDE4抑制剂。 3.一系列新的N-取代的顺-四-和顺-六氢邻苯二氮酮的体内抗炎活性。
2. Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones. [J] . Van-der-Mey M, Hatzelmann A, Van-Klink GP, Journal of Medicinal Chemistry . 2001,第16期

机译：新型选择性PDE4抑制剂。 2.4-芳基取代的顺-四-和顺-六氢邻苯二氮酮的合成和结构-活性关系。
3. Adenosine Kinase Inhibitors. 3. Synthesis, SAR, and Antiinflammatory Activity of a Series of L-Lyxofuranosyl Nucleosides [J] . Bheemarao G. Ugarkar, Angelo J. Castellino, Jay S. DaRe, Journal of Medicinal Chemistry . 2003,第22期

机译：腺苷激酶抑制剂。 3.一系列L-呋喃呋喃糖基核苷的合成，SAR和抗炎活性
4. Synthesis and in vivo antiinflammatory activity of long chain 2-amino-alcohols [C] . Violetta Constantinou-Kokotou, Victoria Magrioti, Dinitra Hadjipavlou-Litina European Peptide Symposium . 2002

机译：长链2-氨基醇的合成和体内抗炎活性
5. Synthesis of boronic acid based sensors for glucose and sialic acid and synthesis of novel and selective PDE4 enzyme inhibitors. [D] . Kaur, Gurpreet. 2006

机译：合成基于硼酸的葡萄糖和唾液酸传感器，以及合成新型选择性PDE4酶抑制剂。
6. A comparison of the inhibitory activity of PDE4 inhibitors on leukocyte PDE4 activity in vitro and eosinophil trafficking in vivo [O] . Nicola Cooper, Mauro M Teixeira, Julie Warneck, 1999

机译：PDE4抑制剂对体外白细胞PDE4活性和体内嗜酸性粒细胞运输的抑制活性比较
7. A comparison of the inhibitory activity of PDE4 inhibitors on leukocyte PDE4 activity in vitro and eosinophil trafficking in vivo [O] . Cooper, Nicola, Teixeira, Mauro M, Warneck, Julie, 1999

机译：PDE4抑制剂对体外白细胞PDE4活性和体内嗜酸性粒细胞运输的抑制活性比较
8. Cellular Regulation of ADP-Ribosylation of Proteins. 3. Selective Augmentation of In vitro ADP-Ribosylation of Histone H3 in Murine Thymic Cells after In vivo Emetine Treatment. [R] . Sooki-Toth, A., Banfalvi, G., Szoelloesi, J., 1989

机译：蛋白质aDp-核糖基化的细胞调节。 3.体内依美舒治疗后小鼠胸腺细胞中组蛋白H3的体外aDp-核糖基化的选择性增强。

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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