Key result
Novel anthranilamide-based FXa inhibitors (compounds 1a, 1g, and 1s) displayed evident FXa inhibitory activity, excellent selectivity over thrombin, and pronounced in vitro anticoagulant activities.
Novel anthranilamide-based compounds demonstrate promising in vitro Factor Xa inhibitory and anticoagulant activities, suggesting potential as future anticoagulant drugs.
These in vitro hits warrant preclinical testing; leaves open development of anthranilamide-based FXa inhibitors.
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.
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Wang et al. (2016) studied Thrombotic diseases. Novel anthranilamide-based FXa inhibitors (compounds 1a, 1g, 1s) was evaluated on FXa inhibitory activity and selectivity over thrombin in vitro. Novel anthranilamide-based FXa inhibitors (compounds 1a, 1g, and 1s) displayed evident FXa inhibitory activity, excellent selectivity over thrombin, and pronounced in vitro anticoagulant activities.
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