novel anthranilamide-based fxa inhibitors: drug design, synthesis and biological evaluation
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ID: 252808
2016
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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.
| Reference Key |
wang2016moleculesnovel
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|---|---|
| Authors | ;Wenzhi Wang;Jing Yuan;Xiaoli Fu;Fancui Meng;Shijun Zhang;Weiren Xu;Yongnan Xu;Changjiang Huang |
| Journal | Journal of ethnopharmacology |
| Year | 2016 |
| DOI |
10.3390/molecules21040491
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| URL | |
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