基于木犀草素结构的氨基醌合成和抗氧化性研究

Synthesis and Antioxidant Activity of Aminoquinones Based on Luteolin Structure

将具有氨基的活性基团引入到木犀草素分子结构中6'位。一是起到增强药效的作用,二是可以对整个分子的脂/水分布系数作一个调整,影响先导化合物的药代动力学参数,以便进行药理试验其抗炎活性。以木犀草素为原料,分别与脂肪胺、醇胺、苄胺等反应,在特定酸度下,经空气氧化及迈克尔加成反应合成较稳定的基于木犀草素结构的氨基醌类化合物。合成步骤较少,反应条件温和,环境污染小。对目标化合物用红外、紫外、核磁共振和质谱等进行结构表征。对产物的抗氧化性及水溶性进行初步研究。

In order to enhance the pharmacologically activity of luteolin,the active group with amino is introduced into the 6＇ position of molecular structure of luteolin.Firstly,it will play a role in enhancing efficacy.Secondly,the entire molecule can be adjusted for the lipid/water distribution coefficient.Hence the pharmacokinetic parameters of the lead compound are affected.Therefore the pharmacological testing of anti-inflammatory activity can be conducted.Luteolin as the raw material,reacted with fatty amine,alcohol amine,benzylamine by continuous reaction of air oxidation and Michael addition at a specific acidity.Relatively stable aminoquinone compounds based on luteolin structure were synthesized.This method had the characteristics of fewer steps,mild reaction conditions and environmentally friendly.The targeted compounds were structurally characterized by IR,UV,NMR and MS.The antioxidant properties and water solubility of the products were studied preliminarily.