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Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.

作者信息

Kleinman E F, Campbell E, Giordano L A, Cohan V L, Jenkinson T H, Cheng J B, Shirley J T, Pettipher E R, Salter E D, Hibbs T A, DiCapua F M, Bordner J

机构信息

Central Research Division, Pfizer Inc., Groton, Connecticut 06340, USA.

出版信息

J Med Chem. 1998 Jan 29;41(3):266-70. doi: 10.1021/jm970685m.

DOI:10.1021/jm970685m
PMID:9464356
Abstract
摘要

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Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.
J Med Chem. 1998 Jan 29;41(3):266-70. doi: 10.1021/jm970685m.
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Modulation of cell adhesion molecule expression and function on human lung microvascular endothelial cells by inhibition of phosphodiesterases 3 and 4.通过抑制磷酸二酯酶3和4对人肺微血管内皮细胞上细胞粘附分子表达和功能的调节
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Airway relaxant and anti-inflammatory properties of a PDE4 inhibitor with low affinity for the high-affinity rolipram binding site.一种对高亲和力咯利普兰结合位点具有低亲和力的磷酸二酯酶4抑制剂的气道舒张和抗炎特性。
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Effects of inhibition of PDE4 and TNF-alpha on local and remote injuries following ischaemia and reperfusion injury.磷酸二酯酶4(PDE4)和肿瘤坏死因子-α(TNF-α)抑制对缺血再灌注损伤后局部和远处损伤的影响。
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SB 207499 (Ariflo), a second generation phosphodiesterase 4 inhibitor, reduces tumor necrosis factor alpha and interleukin-4 production in vivo.SB 207499(阿瑞吡坦),一种第二代磷酸二酯酶4抑制剂,可在体内降低肿瘤坏死因子α和白细胞介素-4的产生。
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1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.1,4-环己烷羧酸酯:用于治疗哮喘的强效且选择性磷酸二酯酶4抑制剂。
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