...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of biomedical materials research. Part B, Applied biomaterials. >Synthesis of monomeric and polymeric conjugates carrying a thrombin inhibitor through an ester bond.
【24h】

Synthesis of monomeric and polymeric conjugates carrying a thrombin inhibitor through an ester bond.

机译：通过酯键携带凝血酶抑制剂的单体和聚合物共轭物的合成。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Four kinds of monomers carrying a thrombin inhibitor, (2R,4R)-4-methyl-1-[N2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl)sulfon yl]-L-arginyl]-2-piperidinecarboxylic acid (argatroban), were synthesized. These monomers were copolymerized with acrylamide to yield water-soluble polymeric conjugates possessing the argatroban moiety in the side chain. Their antithrombogenic activities were determined from the inhibitory effect on thrombin action and the prolongation effect on blood clotting time. The monomeric conjugates of 2-hydroxyethyl acrylate (HEA), 2-hydroxyethyl methacrylate (HEMA), and 4-hydroxybutyl acrylate (HBA) linked with argatroban through an ester bond were potent inhibitors of thrombin, prolonging the blood-clotting time, whereas a conjugate of amino methyl styrene (AMS) and argatroban through an amide bond was a less potent inhibitor than argatroban. None of the copolymers could prolong blood clotting when assessed just after preparation of their aqueous solutions, but the antithrombogenic activity of the aqueous solutions increased after incubation for 7 days at 37 degrees C for the polymeric conjugates through an ester bond. Free argatroban was detected in the aqueous solutions of polymeric conjugates after incubation, suggesting that argatroban was released by hydrolysis of the ester bond during incubation.
机译：带有凝血酶抑制剂的四种单体，（2R，4R）-4-甲基-1- [N2-[（3-甲基-1,2,3,4-四氢-8-喹啉基）磺酰基] -L-合成了精氨酸基] -2-哌啶甲酸（argatroban）。这些单体与丙烯酰胺共聚，得到在侧链上具有argatroban部分的水溶性聚合物共轭物。通过对凝血酶的抑制作用和对凝血时间的延长作用来确定它们的抗血栓形成活性。通过酯键与argatroban相连的丙烯酸2-羟乙酯（HEA），甲基丙烯酸2-羟乙酯（HEMA）和丙烯酸4-羟丁酯（HBA）的单体共轭物是凝血酶的有效抑制剂，延长了凝血时间，而氨基甲基苯乙烯（AMS）和Argatroban通过酰胺键的共轭物比Argatroban的抑制作用更弱。刚制备完水溶液后进行评估时，没有一种共聚物可以延长血液凝结，但是通过酯键在37℃下孵育7天后，水溶液的抗血栓形成活性增加。孵育后在聚合物结合物的水溶液中检测到游离的argatroban，这表明孵育期间argatroban通过酯键的水解而释放。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号