Synthesis and ionophoric activities of functionalized bis(choloyl) conjugates with a rigid core |
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Authors: | Jia Zhou Yong-Ming Lu Li-Qun Deng Zhong-Zhen Zhou Wen-Hua Chen |
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Institution: | School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China |
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Abstract: | Three bis(choloyl) conjugates bearing a rigid p-phenylenediamine/p-bis(aminomethyl)benzene linker and amino/acetamido groups were synthesized, and fully characterized on the basis of 1H NMR, ESI-MS and HRMS. Their ionophoric activities were investigated by means of pH discharge assay. The results indicate that these conjugates exhibit potent ionophoric activities across egg-yolk l-α-phosphatidylcholine (EYPC)-based liposomal membranes, via a cation/proton antiport mechanism. They show moderate ion selectivity among alkali metal ions. Of the three conjugates, the ones having amino groups transport alkali metal ions in the order of Na+ > Li+ > K+ ≈ Rb+ ≈ Cs+, whereas the one having acetamido groups functions in the order of Li+ > Na+ > K+ ≈ Rb+ ≈ Cs+. |
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Keywords: | Ionophore Choloyl conjugate Synthesis pH Discharge |
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