Synthesis of (2E)-3-{2-[(substituted benzyl)oxy]phenyl}acrylaldehydes as novel anti-inflammatory agents.
作者： Li-Jiau Huang , Jih-Pyang Wang , Yu-Chi Lai , Sheng-Chu Kuo
DOI: 10.1016/J.BMCL.2006.02.005
关键词: Lead compound 、 Chemistry 、 Biological activity 、 Anti-inflammatory 、 Aldehyde 、 Stereochemistry 、 Chemical synthesis 、 Trifluoperazine 、 Superoxide 、 Mechanism of action
摘要: Abstract As part of our continuing effort for development novel anti-inflammatory agents, the highly potential agent CCY1a, which we reported recently, was selected as lead compound to synthesize a series its derivatives evaluation. Most newly synthesized compounds exhibited superior inhibitory activity than both and positive control (trifluoperazine) toward fMLP-stimulated neutrophil superoxide formation. (2E)-3-[2-(Benzyloxy)-5-methoxyphenyl]-acrylaldehyde (31) among most potent with action mechanism different from CCY1a in that it does not act cAMP-elevating but inhibits increase cellular Ca2+ greater potency.
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