Li Zhi, Deng Li-Qun, Chen Yun, Wu Tao, Chen Wen-Hua
Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
Bioorg Med Chem Lett. 2016 Aug 1;26(15):3665-8. doi: 10.1016/j.bmcl.2016.05.089. Epub 2016 Jun 1.
A bis(imidazolyl)-functionalized bis(choloyl) conjugate was synthesized and assessed for its transmembrane anionophoric activity by means of chloride ion selective electrode technique and pyranine assays. The results indicate that under the assay conditions, this conjugate was capable of mediating the symport of proton and anions, presumably via a channel mechanism. In addition, this compound was found to exhibit much higher anionophoric activity than the analogue without imidazolyl groups, revealing the significant role of the imidazolyl groups in the anion transport process.
合成了一种双(咪唑基)功能化的双(胆酰基)共轭物,并通过氯离子选择性电极技术和吡喃荧光素测定法评估其跨膜阴离子载体活性。结果表明,在测定条件下,该共轭物能够介导质子和阴离子的同向转运,推测是通过通道机制实现的。此外,发现该化合物比没有咪唑基的类似物表现出更高的阴离子载体活性,揭示了咪唑基在阴离子转运过程中的重要作用。