Synthesis of (2E)-3-{2-[(substituted benzyl)oxy]phenyl}acrylaldehydes as novel anti-inflammatory agents |
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Authors: | Huang Li-Jiau Wang Jih-Pyang Lai Yu-Chi Kuo Sheng-Chu |
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Affiliation: | Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung 40402, Taiwan, ROC. ljhuang@mail.cmu.edu.tw |
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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. |
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