【摘要】 目的合成选择性中性白细胞弹性蛋白酶抑制剂西维来司钠的衍生物,并探讨其生物活性。方法采用4条不同的反应路线,以改善西维来司钠在水中的溶解性为出发点,合成4类未见文献报道的西维来司钠类似物,并考察其在水中的溶解性。结果与结论设计并合成了4类13个未见文献报道的西维来司钠类似物,结构经IR1、H-NMR、MS分析确证。除Ⅲ类、化合物Ⅱ2外,其余化合物在水中的溶解性均得到明显的改善。初步的体外弹性蛋白酶抑制活性实验显示:所合成的化合物均具有一定的弹性蛋白酶抑制作用。Ⅱ4和Ⅲ1的抑制活性优于其他化合物,分别为85.6%和85.3%。更多还原

【Abstract】 Aim To study the synthesis and biological activities of several sivelast sodium analogues.Methods Thirteen new target molecules with better solubility were designed and synthesized.Neutrophil elastase inhibition ability was tested.Results and conclusion The structures of the analogues were confirmed by IR,（）¹H-NMR and MS.Except type Ⅲ and compound Ⅱ₂,all derivatives are soluble in water,and also have improved solubility in most organic solvent.The preliminary pharmacological in vitro test showed that all compounds have inhibition effect on elastase.Among them,Ⅱ₄ and Ⅲ₁ are excellent than others（85.6% and 85.3%,respectively）.Further pharmacological experiments are to be continued.更多还原