摘要
目的设计合成未见文献报道的α 取代肉桂酰苯乙胺类化合物 ,并对其进行生物活性筛选。方法在肉桂酸部分的苯环上 ,分别引入 p Cl、3,4 OCH2 O、p NO2 等取代基 ,而在苯乙胺部分的苯环上 ,对邻位和间位用甲氧基进行取代 ,先后合成了 18个α 取代肉桂酰苯乙胺类化合物 ,结构经元素分析、HREIMS、EI MS、1H NMR、IR确认。结果目标化合物具有明显的免疫及舒张血管的活性。结论该类化合物作为药物先导化合物 ,具有进一步研究的价值。
Aim Some novel α substituted N (phenylethyl)cinnamides were designed and synthesized,and their bioactivity were evaluated.Methods Eighteen title compounds were synthesized successfully and were identified by element analysis HERIMS EI MS 1H NMR IR,and several bioassay systems were used to evaluate their bioactivity.Results The title compounds showed remarkable immunity and vasodilating effects.Conlusion α Substituted n (phenylethyl)cinnamides are worth further studying as the new leading drug.
出处
《中国药物化学杂志》
CAS
CSCD
2003年第6期329-334,355,共7页
Chinese Journal of Medicinal Chemistry
关键词
药物化学
制备
化学合成
α-取代肉桂酰苯乙胺
免疫活性
扩血管活性
medicinal chemistry
preparation
chemical synthesis
αsubstituted N(phenylethyl)cinnamides
immunity activity
vasodilative activity