噁唑烷酮醚类化合物的合成及其Ⅹa因子抑制活性  

Synthesis and evaluation of oxazolidinone ether compounds as factor Xa inhibitors

作　　者：李慧[1] 杨凌云[1] 周金培[1] 张惠斌[1] 

机构地区：[1]中国药科大学新药研究中心,南京210009

出　　处：《中国药科大学学报》2013年第5期385-389,共5页Journal of China Pharmaceutical University

基　　金：国家“重大新药创制”科技重大专项资助项目(No.2013ZX09301303-002);江苏省产学研联合创新资金-前瞻性联合研究项目(No.BY2011158);中央高校基本科研业务费专项基金资助项目(No.JKY2011092)~~

摘　　要：以利伐沙班结构为基础,根据其与Ⅹa因子相互作用的特点对其进行结构改造,设计并合成了一系列未见报道的唑烷酮醚类化合物(7a^7m)。所合成化合物结构均经IR,1H NMR和MS确证,并测定了目标衍生物Ⅹa因子抑制活性。实验数据表明,所合成化合物均表现出了一定的Ⅹa因子抑制活性,但活性低于利伐沙班。According to the binding mode of rivaroxaban in complex with human factor Xa and the chemical structure of rivaroxaban, we have designed and synthesized the oxazolidinone ether compounds, which have not be reported in literatures. The structures of all the rivaroxaban derivatives synthesized were identified by IR, 1 H NMR and MS. The anti-factor Xa activity of the synthesized compounds was tested. The results showed that all of the tested compounds exhibited some activity, yet were less potent than rivaroxaban.

关 键 词：噁唑烷酮醚类化合物 利伐沙班 衍生物 合成 Ⅹa因子抑制剂 抑制活性 

分 类 号：R914[医药卫生—药物化学] R965[医药卫生—药学]