Synthesis of novel trans-stilbene derivatives and evaluation of their potent antioxidant and neuroprotective effects
作者:Jae-Chul Jung、Eunyoung Lim、Yongnam Lee、Jun-Mo Kang、Heejeong Kim、Soyong Jang、Seikwan Oh、Mankil Jung
DOI:10.1016/j.ejmech.2009.03.011
日期:2009.8
biological properties of new amides, esters and other derivatives of trans-stilbene are described. The key synthetic strategies involve the Wittig–Horner reaction of a phosphonium salt 9 and an aldehyde 10 to generate (E)- or (Z)-olefins and a coupling reaction of an acid 12 and various amines 13a–n to give trans-stilbene derivatives 15a–n in high yields. A amide derivative 15g showed three times more in
描述了反式二苯乙烯的新酰胺,酯和其他衍生物的方便合成及其生物学特性。键合成策略涉及鏻盐的Wittig-Horner反应9和醛10,以产生(ë) -或(Ž)烯烃和酸的偶合反应12和各种胺13A - Ñ,得到反式-芪高产率的衍生物15a – n。15克酰胺衍生物在体外显示出三倍的增长清除自由基的活性高于白藜芦醇,而另外15d对脂多糖(LPS)a诱导的NO生成则显示出强大的抑制活性。烯丙基酰胺类似物15a在谷氨酸诱导的原代皮层神经元细胞中显示出最有效的神经保护活性。