Design, synthesis and biological evaluation of novel 2,3-dihydroquinazolin- 4(1H)-one derivatives as potential fXa inhibitors

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• 作者：Junhao Xing^a ; ^{xingjhcpu@163.com} ; Lingyun Yang^a ; Yifei Yang^a ; Leilei Zhao^a ; Qiangqiang Wei^b ; Jian Zhang^a ; Jinpei Zhou^b ; Huibin Zhang^a ; ^c ; ^{zhanghb80@163.com} ; ^{hb_zhang@hotmail.com}
• 关键词：Factor Xa ; Anticoagulant ; fXa inhibitor ; Arteriovenous shunt ; Bleeding risk ; Thromboembolic diseases
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：411-422
• 全文大小：2028 K
• 卷排序：125

文摘

Three series of 2,3-dihydroquinazolin-4(1H)-one derivatives were prepared. Most of the compounds had significant fXa inhibitory activity. 8e exhibited the strongest potency against fXa and good selectivity versus thrombin. 8e also displayed great in vitro and in vivo antithrombotic activity. 8e had a similar safety profile on bleeding risk as that of betrixaban.