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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
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Synthesis and factor Xa inhibitory activity of apixaban derivatives

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  • 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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