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CHOLIC ACID MODIFIED GLUCOSAMINE DERIVATIVE AND PREPARATION METHOD AND USE

机译:胆酸修饰的葡萄糖胺衍生物的制备及使用方法

摘要

The present invention relates to a cholic acid modified glucosamine derivative and a preparation method and use therefor, the derivative being as shown in formula (I), wherein R1 is H or OH, R2 is H or OH, R3 is H, CH2 = CHCO- or CH2 = C(CH3)CO-. In the presence of a carbodiimide condensation reagent, reacting the cholic acid with excess acid N- hydroxysuccinimide or 1-hydroxybenzotriazole generates an cholic acid active ester, and then reacting with D- glucosamine to obtain a derivative without polymerizable groups; or first reacting the cholic acid active ester with acyl chloride containing vinyl, and then reacting with D- glucosamine to obtain a derivative with polymerizable groups. The derivative of the present invention has a good biocompatibility, the derivative without polymerizable groups can be used as a medicine for the treatment of osteoarthritis, and the derivative with polymerizable groups is an organic matrix for a cartilage prosthesis material, or for constructing in situ molded glucosamine functional hydrogels.
机译:本发明涉及一种胆酸修饰的葡糖胺衍生物及其制备方法和用途,该衍生物如式(I)所示,其中R 1为H或OH,R 2为H或OH,R 3为H,CH 2 = CHCO -或CH2 = C(CH3)CO-。在碳二亚胺缩合剂的存在下,使胆酸与过量的酸N-羟基琥珀酰亚胺或1-羟基苯并三唑反应,生成胆酸活性酯,然后与D-葡糖胺反应,得到不具有可聚合基团的衍生物。或首先使胆酸活性酯与含有乙烯基的酰氯反应,然后与D-葡糖胺反应以获得具有可聚合基团的衍生物。本发明的衍生物具有良好的生物相容性,不具有可聚合基团的衍生物可以用作治疗骨关节炎的药物,具有可聚合基团的衍生物是用于软骨假体材料或用于原位成型的有机基质。氨基葡萄糖功能水凝胶。

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