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邢峻豪, 张媛, 胡晓雯, 周金培, 张惠斌. 阿哌沙班衍生物的合成及Ⅹa因子抑制活性[J]. 中国药科大学学报, 2013, 44(4): 289-295. DOI: 10.11665/j.issn.1000-5048.20130401
引用本文: 邢峻豪, 张媛, 胡晓雯, 周金培, 张惠斌. 阿哌沙班衍生物的合成及Ⅹa因子抑制活性[J]. 中国药科大学学报, 2013, 44(4): 289-295. DOI: 10.11665/j.issn.1000-5048.20130401
XING Junhao, ZHANG Yuan, HU Xiaowen, ZHOU Jinpei, ZHANG Huibin. Synthesis and factor Xa inhibitory activity of apixaban derivatives[J]. Journal of China Pharmaceutical University, 2013, 44(4): 289-295. DOI: 10.11665/j.issn.1000-5048.20130401
Citation: XING Junhao, ZHANG Yuan, HU Xiaowen, ZHOU Jinpei, ZHANG Huibin. Synthesis and factor Xa inhibitory activity of apixaban derivatives[J]. Journal of China Pharmaceutical University, 2013, 44(4): 289-295. DOI: 10.11665/j.issn.1000-5048.20130401

阿哌沙班衍生物的合成及Ⅹa因子抑制活性

Synthesis and factor Xa inhibitory activity of apixaban derivatives

  • 摘要: 在阿哌沙班的结构基础上,保持其P1部分不变,对其P4部分进行结构改造,用一系列芳香酰胺基团代替2-氮己酮,合成了一系列未见报道的吡唑并吡啶酮类化合物。所合成化合物结构均经IR,1H NMR和MS确证,并对这些化合物的Ⅹa因子抑制活性进行了测定,结果表明所有化合物均表现出一定的Ⅹa因子抑制活性,但活性均低于阳性药阿哌沙班。

     

    Abstract: Based on the current structure-activity relationship of apixaban, keeping P1 portions unchanged and replace δ-valerolactam in P4 portions with aromatic amide group, a series of dihydropyrazolopyridinones not reported were designed and synthesized. The structures of all the synthesized derivatives were identified by IR, 1H NMR and MS. And then their anti-factor Xa activity was tested. The results showed that all the tested compounds exhibited factor Xa inhibitory activity, but with less potency than that of apixaban.

     

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