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目的合成以含有Asp-Glu片段的寡肽为载体的非甾体抗炎前药,并初步研究其骨靶向性。方法使用混合酸酐法制备(Asp-Glu)n-Nap前药,通过HAP法研究其骨靶向性。结果制备得到(Asp-Glu)n-Nap前药,产物经ESI-MS和1HNMR确证。HAP实验显示较好的体外骨靶向性。结论所用方法可行,制备的(Asp-Glu)n-Nap非甾体抗炎前药具有潜在的骨靶向性。
Objective To synthesize non-steroidal anti-inflammatory pro-drugs with oligopeptides containing Asp-Glu fragments as carriers and to study their bone targeting. Methods (Asp-Glu) n-Nap prodrug was prepared by a mixed anhydride method and its bone targeting was studied by HAP method. As a result, (Asp-Glu) n-Nap prodrug was prepared and the product was confirmed by ESI-MS and 1HNMR. HAP experiments show better in vitro bone targeting. Conclusion The method is feasible. The prepared (Asp-Glu) n-Nap NSAIDs have potential bone targeting.