"特洛伊木马"型CMP-KDO合成酶抑制剂前药的设计与合成
esign and synthesis of "Trojan horse" type CMP-KDO synthase inhibitor prodrug
MP-KDO合成酶抑制剂有望成为新型抗革兰氏阴性菌的抗菌药,其中很多活性分子由于其高极性导致其不能跨膜进入细菌。为了解决这一难题,本文以铁载体型"特洛伊木马"抗菌偶联物为设计概念,设计了一个前药型铁载体抗菌缀合物。该缀合物由铁载体、连接臂以及活性物质(KDO衍生物)三部分组成。利用该策略,本文成功合成了一个前药型铁载体抗菌缀合物。
MP-KDO synthase inhibitors are promising as novel antimicrobials against gram-negative bacteria, many of which are active molecules that cannot cross the membrane due to their high polarity.In order to solve this problem, this paper designed a prodrug iron carrier antimicrobial conjugate based on the design concept of iron carrier "Trojan horse" antimicrobial conjugate.The conjugate consists of three parts: iron carrier, linkage arm and active substance (KDO derivative).Using this strategy, a prodrug type iron carrier conjugate was successfully synthesized.
梁晟辉、贺耘、郭键
药学生物化学分子生物学
药物化学抗菌缀合物铁载体MP-KDO合成酶
pharmaceutical chemistryantibacterial conjugatesSiderophoreCMP-KDO synthase
梁晟辉,贺耘,郭键."特洛伊木马"型CMP-KDO合成酶抑制剂前药的设计与合成[EB/OL].(2021-04-09)[2025-08-16].http://www.paper.edu.cn/releasepaper/content/202104-84.点此复制
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