Synthesis and antioxidative/anti-inflammatory activity of novel fullerene–polyamine conjugates
作者:George E. Magoulas、Thomas Garnelis、Constantinos M. Athanassopoulos、Dionissios Papaioannou、George Mattheolabakis、Konstantinos Avgoustakis、Dimitra Hadjipavlou-Litina
DOI:10.1016/j.tet.2012.06.066
日期:2012.9
(E)-4-(Fullerenopyrrolidin-1-yl)-3-methylbut-2-enoic acid and its corresponding succinimidyl ester, readily obtained through Prato-type modification of C-60, were used for the selective N-acylation of polyamines. The thus obtained conjugates were evaluated for their antioxidative and anti-inflammatory activity and their cytotoxicity was determined. Members of this family of compounds showed interesting anti-lipid peroxidation, anti-lipoxygenase and anti-inflammatory activity and comparable cytocompatibility to spermidine. (C) 2012 Elsevier Ltd. All rights reserved.
(E)-4-(富勒烯吡咯基)-3-甲基丁二烯酸和对应的丙二酸 succeedinimidyl 酯通过普拉托型修饰C-60易得,被广泛应用于富选择性N-酰化反应。由此获得的共轭体被评估为抗氧化及抗炎活性,同时测定它们的细胞毒性。本系列化合物显示出令人感兴趣的抗脂过氧化、抗氧酶活性及抗炎活性,且与苏丹类物质相比具有相近的细胞相容性。(C)2012 Elsevier Ltd. All rights reserved.