芳基乙酸类衍生物的设计、合成与抗过敏活性研究

Design, Synthesis and Anti-Allergic Activity Evaluation of Aryl-Acetic Acid Derivatives

目的:为了获得活性好、副作用小的DP受体拮抗剂,设计和合成芳基乙酸类衍生物。方法:以取代的苯酚、1,2-二溴乙烷以及香豆酸为原料,通过醚化、水解、酰胺化、水解等反应合成目标化合物,并研究其对烟酸诱导血管扩张效应的抑制活性。结果:合成了5个目标化合物,活性筛选结果表明,化合物I-4和I-5的活性优于阳性药(拉罗匹仑)。结论:化合物I-4和I-5对烟酸引起的血管扩张具有抑制作用,值得进一步研究。

Objective: To discover novel DP receptor antagonists with higher potency and less side-effect, several arylacetic acid derivatives were designed and synthesized. Method: A series of title com-pounds were synthesized by etherification, hydrolysis, amidation and hydrolysis on the basis of substitutional phenol, 1,2-dibromoethane and coumarate. All the target compounds were evaluated by the model of niacin-induced vasodilation. Results: 5 title compounds were synthesized. The results of biological evaluation showed that the compounds I-4 and I-5 exhibited more potency than positive drug (Laropiprant). Conclusion: The compounds I-4 and I-5 showed potent inhibitory effect on niacin-induced vasodilation and would be valuable for further investigation.