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, 14 (4), 989-93

Design, Synthesis, and SAR of Anthranilamide-Based Factor Xa Inhibitors With Improved Functional Activity

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Design, Synthesis, and SAR of Anthranilamide-Based Factor Xa Inhibitors With Improved Functional Activity

Penglie Zhang et al. Bioorg Med Chem Lett.

Abstract

Compound 2 containing an aminomethylbenzoyl moiety as the S4 binding motif was synthesized in order to modulate hydrophlicity of anthranilamide-based factor Xa inhibitors with substituted biphenyl P4 groups. Structure-activity relationship studies around 2 have led to a series of potent factor Xa inhibitors which are highly active in the human plasma-based thrombin generation assay with 2XTG values less than 1 microM. Compound 55 shows strong antithrombotic activity in our rabbit deep vein thrombosis model, and also exhibits good oral bioavailability and a long half life in rats.

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