Novel 3-oxa lipoxin A4 analogues with enhanced chemical and metabolic stability have anti-inflammatory activity in vivo

…, C Mallari, J Terkelsen, JL Tseng, J Shen…

文献索引：Guilford, William J.; Bauman, John G.; Skuballa, Werner; Bauer, Shawn; Wei, Guo Ping; Davey, David; Schaefer, Caralee; Mallari, Cornell; Terkelsen, Jennifer; Tseng, Jih-Lie; Shen, Jun; Subramanyam, Babu; Schottelius, Arndt J.; Parkinson, John F. Journal of Medicinal Chemistry, 2004 , vol. 47, # 8 p. 2157 - 2165

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被引用次数: 56

摘要

Lipoxin A4 (LXA4) is a structurally and functionally distinct natural product called an eicosanoid, which displays immunomodulatory and anti-inflammatory activity but is rapidly metabolized to inactive catabolites in vivo. A previously described analogue of LXA4, methyl (5 R, 6 R, 7 E, 9 E, 11 Z, 13 E, 15 S)-16-(4-fluorophenoxy)-5, 6, 15-trihydroxy-7, 9, 11, 13- hexadecatetraenoate (2, ATLa), was shown to have a poor pharmacokinetic profile after ...