Abstract
(E)-3,4-dihydroxystyryl p-substituted-phenethyl ketones and their 3,4-diacetylated derivatives were synthesized and examined their neuroprotective activities to further study the effect of p-substituents on the aromatic ring. The results revealed that steric hindrance effect of p-substituents has impact on neuroprotective activities against inflammatory and oxidative injury. Introduction of the bulkier groups are more beneficial to improve the neuroprotective activities than smaller groups. Compounds (4–5h, 4–5i and 4–5e) with p-substituted trifluoromethyl, isopropyl and t-butyl groups exhibited the best effects among all the target compounds.
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This study was supported by the National Natural Science Foundation of China (Grant Nos. 20972011, 21042009 and 21172014) and Ministry of Science and Technology of China (2009ZX09301-010).
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Cheng, C., Ning, X., Luo, Y. et al. Synthesis and neuroprotective evaluation of (E)-3,4-dihydroxystyryl p-substituted-phenethyl ketone derivatives against inflammatory and oxidative injury. Med Chem Res 25, 1678–1685 (2016). https://doi.org/10.1007/s00044-016-1601-3
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DOI: https://doi.org/10.1007/s00044-016-1601-3