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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
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Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.

机译:5-氨基水杨酸互偶氮前药在炎症性肠病中结肠特异性药物递送的合成,动力学研究和药理学评价。

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摘要

Mutual azo prodrug of 5-aminosalicylic acid with l-tyrosine was synthesized by coupling l-tyrosine with salicylic acid, for targeted drug delivery to the inflamed gut tissue in inflammatory bowel disease. The structure was confirmed by elemental analysis, IR and NMR spectroscopy. In vitro kinetic studies in rat fecal matter showed 87.18% release of 5-aminosalicylic acid with a half-life of 140.28min, following first order kinetics. Therapeutic efficacy of the carrier system and the mitigating effect of the azo conjugate were evaluated in trinitrobenzenesulfonic acid-induced experimental colitis model. Myeloperoxidase activity was determined by the method of Krawisz et al. The synthesized prodrug was found to produce comparable mitigating effect as that of sulfasalazine on colitis in rats.
机译:通过将L-酪氨酸与水杨酸偶联,合成5-氨基水杨酸与L-酪氨酸的偶氮前药,用于将药物靶向递送至炎性肠病中的发炎的肠组织。通过元素分析,IR和NMR光谱确认结构。在大鼠粪便中的体外动力学研究表明,遵循一级动力学,5-氨基水杨酸的释放率为87.18%,半衰期为140.28min。在三硝基苯磺酸诱导的实验性结肠炎模型中评估了载体系统的治疗功效和偶氮偶联物的缓解作用。髓过氧化物酶活性通过Krawisz等人的方法测定。发现合成的前药可产生与柳氮磺胺吡啶对大鼠结肠炎相当的缓解作用。

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