基于D-苯丙氨酸骨架的萘普生类似物的合成及其对COX-2的选择性研究

Synthesis of Naproxen Analogs Based on D-Phenylalanine Skeleton and Its Selectivity to COX-2

为了研究和开发安全有效且副作用小的抗炎药物,设计和合成了一系列基于D-苯丙氨酸骨架的萘普生类似物,通过氢谱及碳谱数据确证目标产物的结构,并采用MTT法和免疫荧光法分别测定目标化合物对RAW 264.7细胞的毒性和对COX-2的选择能力。结果显示系列目标化合物的细胞毒性数据与萘普生的相当,目标化合物3对COX-2具有较好的选择性。

In order to research and develop safe and effective anti-inflammatory drugs with small side effects,a series of naproxen analogs based on D-phenylalanine skeleton were designed and synthesized.The structure of the target product was confirmed by NMR.The toxicity of the target product to RAW 264.7 cells and the ability to select COX-2 were measured by MTT method and immunofluorescence method.The results show that the cytotoxicity data of a series of target compounds are comparable to those of naproxen,and target compound 3 has good selectivity for COX-2.