Synthesis and evaluation of anthranilamide-based derivatives as FXa inhibitors
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Changjiang Huang1,2, Wenzhi Wang3, Yao Li2, Shijun Zhang2, Fancui Meng2, Weiren Xu2, Jing Yuan2, Ligong Chen1,4,5
1School of Chemical Engineering and Technology, Tianjin University, Tianjin, China
2Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin, China
3School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, China
4Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, China
5Tianjin Engineering Research Center of Functional Fine Chemicals, Tianjin, China
Jing Yuan, email: [email protected]
Ligong Chen, email: [email protected]
Keywords: thrombosis, thromboembolic diseases, anticoagulants, factor Xa inhibitors, thrombin and docking simulation
Received: November 23, 2016 Accepted: March 10, 2017 Published: March 21, 2017
Factor Xa (FXa) plays a significant role in the blood coagulation cascade and is a promising target for anticoagulation drugs. Three oral FXa inhibitors have been approved by FDA for treating thrombotic diseases. In this study, 43 novel compounds were synthesized anthranilamide-based FXa inhibitors aiming to ameliorate the toxicity of traditional FXa inhibitors in clinic. The data indicated that the compounds 6a, 6a-b, 6a-e, 6k, 6k-a and 6k-b showed remarkable FXa inhibitory activity and excellent selectivity over thrombin in vitro. Selected compounds also exhibited anticoagulant activities in vitro consequently and were potent novel anti-coagulators in further.
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