作者:Denis S. Baranov、Anna S. Smorygina、Sergei A. Dzuba
DOI:10.3390/molecules27134127
日期:——
be applied to study its interaction with biological membranes and proteins if its spin-labeled analogs were synthesized. Here, a simple sequence of ibuprofen transformations—nitration, esterification, reduction, Sandmeyer reaction, Sonogashira cross-coupling, oxidation and saponification—was developed to attain this goal. The synthesis resulted in spin-labeled ibuprofen (ibuprofen-SL) in which the spin
布洛芬是一种非甾体抗炎药,具有镇痛和解热活性。如果合成了其自旋标记的类似物,则可以应用电子顺磁共振 (EPR) 光谱来研究其与生物膜和蛋白质的相互作用。在这里,开发了布洛芬转化的简单序列——硝化、酯化、还原、Sandmeyer 反应、Sonogashira 交叉偶联、氧化和皂化——来实现这一目标。该合成产生了自旋标记的布洛芬 (ibuprofen-SL),其中自旋标记 TEMPOL 连接到苯环上。EPR 光谱证实了布洛芬-SL 与 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) 双层的相互作用。使用2H 电子自旋回波包络调制 (ESEEM) 光谱,发现布洛芬-SL 嵌入疏水双层内部。