apixaban and 1-2-4-triazole

apixaban has been researched along with 1-2-4-triazole* in 1 studies

Other Studies

1 other study(ies) available for apixaban and 1-2-4-triazole

Article	Year
Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element. Bioorganic & medicinal chemistry, 2016, 11-01, Volume: 24, Issue:21 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 IC Topics: Animals; Binding Sites; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Design; Factor Xa; Factor Xa Inhibitors; Humans; Models, Molecular; Molecular Structure; Pyrazoles; Pyridones; Pyrroles; Rabbits; Rats; Structure-Activity Relationship; Triazoles; Venous Thrombosis	2016

Article

Year

Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element.

Bioorganic & medicinal chemistry, 2016, 11-01, Volume: 24, Issue:21

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 IC

Topics: Animals; Binding Sites; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Design; Factor Xa; Factor Xa Inhibitors; Humans; Models, Molecular; Molecular Structure; Pyrazoles; Pyridones; Pyrroles; Rabbits; Rats; Structure-Activity Relationship; Triazoles; Venous Thrombosis

2016