Bioorganic and Medicinal Chemistry p. 5646 - 5661 (2016)
Update date:2022-08-05
Topics:
Wang, Yong
Sun, Xiaoqing
Yang, Di
Guo, Zhuang
Fan, Xuxu
Nie, Minhua
Zhang, Feng
Liu, Yue
Li, Yue
Wang, Yulin
Gong, Ping
Liu, Yajing
Four series of novel and potent FXa inhibitors possessing the 1,2,4-triazole moiety and pyrrole moiety as P2 binding element and dihydroimidazole/tetrahydropyrimidine groups as P4 binding element were designed, synthesized, and evaluated for their anticoagulant activity in human and rabbit plasma in vitro. Most compounds showed moderate to excellent activity. Compounds 14a, 16, 18c, 26c, 35a, and 35b were further examined for their inhibition activity against human FXa in vitro and rat venous thrombosis in vivo. The most promising compound 14a, with an IC50(FXa) value of 0.15?μM and 99% inhibition rate, was identified for further evaluation as an FXa inhibitor.
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