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Synthesis and evaluation of anthranilamide-based derivatives as FXa inhibitors.

ABSTRACT: 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.

SUBMITTER: Huang C 

PROVIDER: S-EPMC5514901 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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Synthesis and evaluation of anthranilamide-based derivatives as FXa inhibitors.

Huang Changjiang C   Wang Wenzhi W   Li Yao Y   Zhang Shijun S   Meng Fancui F   Xu Weiren W   Yuan Jing J   Chen Ligong L  

Oncotarget 20170601 23

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 excelle  ...[more]

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