甘氨酸修饰异丙酸类NSAIDs化合物的合成及其对COX-2的选择性研究

Synthesis of Glycine Modified Isopropionic Acid NSAIDs and Its Selectivity to COX-2

为了得到药效良好且副作用小的抗炎药物,通过甘氨酸对异丙酸类NSAIDs进行结构修饰,设计、合成得到目标化合物,通过核磁共振分析表征目标化合物的结构,通过MTT法测定目标化合物对RAW 264.7细胞的毒性,通过免疫荧光法测定目标化合物对COX-2的选择能力。结果显示合成的目标化合物的细胞毒性数据与布洛芬、酮洛芬的相当,与布洛芬、酮洛芬相比对COX-2具有较好的选择性。

In order to obtain potent anti-inflammatory drugs,the novel isopropionic acid derivatives containing glycine were designed and synthesized.Nuclear Magnetic Resonance(NMR)data revealed that the target compounds were successfully synthesized.Characterized.The biological evaluation of target compounds was measured by MTT method and immunofluorescence method.These results showed that the cytotoxicity data of the target compound is comparable to that of ibuprofen or ketoprofen,and the target compounds have better selectivity to cyclooxygenase-2(COX-2)than ibuprofen and ketoprofen.