Synthesis of (2E)-3-{2-[(substituted benzyl)oxy]phenyl}acrylaldehydes as novel anti-inflammatory agents.

Basic Information

ID: ALA1147710

Journal: Bioorg Med Chem Lett

Title: Synthesis of (2E)-3-{2-[(substituted benzyl)oxy]phenyl}acrylaldehydes as novel anti-inflammatory agents.

Authors: Huang LJ, Wang JP, Lai YC, Kuo SC.

Abstract: As part of our continuing effort for development of novel anti-inflammatory agents, the highly potential agent CCY1a, which we reported recently, was selected as lead compound to synthesize a series of its derivatives for evaluation. Most of the newly synthesized compounds exhibited superior inhibitory activity than both the lead compound and the positive control (trifluoperazine) toward fMLP-stimulated neutrophil superoxide formation. (2E)-3-[2-(Benzyloxy)-5-methoxyphenyl]-acrylaldehyde (31) was among the most potent with action mechanism different from CCY1a in that it does not act as cAMP-elevating agent but inhibits the increase in cellular Ca(2+) with greater potency.

CiteXplore: 16510283

DOI: 10.1016/j.bmcl.2006.02.005

Patent ID: