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Molecules 2016, 21(4), 491; doi:10.3390/molecules21040491

Novel Anthranilamide-Based FXa Inhibitors: Drug Design, Synthesis and Biological Evaluation

1
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
2
Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 2 February 2016 / Revised: 31 March 2016 / Accepted: 7 April 2016 / Published: 14 April 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [2874 KB, uploaded 14 April 2016]   |  

Abstract

Factor Xa (FXa) plays a significant role in the blood coagulation cascade and it has become a promising target for anticoagulation drugs. Three oral direct FXa inhibitors have been approved by the FDA for treating thrombotic diseases. By structure-activity relationship (SAR) analysis upon these FXa inhibitors, a series of novel anthranilamide-based FXa inhibitors were designed and synthesized. According to our study, compounds 1a, 1g and 1s displayed evident FXa inhibitory activity and excellent selectivity over thrombin in in vitro inhibition activities studies. Compounds 1g and 1s also exhibited pronounced anticoagulant activities in in vitro anticoagulant activity studies. View Full-Text
Keywords: thrombosis; FXa inhibitor; anthranilamide-based FXa inhibitors; docking simulation thrombosis; FXa inhibitor; anthranilamide-based FXa inhibitors; docking simulation
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Wang, W.; Yuan, J.; Fu, X.; Meng, F.; Zhang, S.; Xu, W.; Xu, Y.; Huang, C. Novel Anthranilamide-Based FXa Inhibitors: Drug Design, Synthesis and Biological Evaluation. Molecules 2016, 21, 491.

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