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Design, Synthesis and Biological Evaluation of Anthranilamide Derivatives as Potential Factor Xa (fXa) Inhibitors

Design, Synthesis and Biological Evaluation of Anthranilamide Derivatives as Potential Factor Xa (fXa) Inhibitors

Junhao Xing, Lingyun Yang, Jinpei Zhou, Huibin Zhang

Bioorg Med Chem. 2018 Dec 15;26(23-24):5987-5999.

PMID: 30446438

Abstract:

Factor Xa (fXa) is a crucial player in various thromboembolic disorders. Inhibition of fXa can provide safe and effective antithrombotic effects. In this study, a series of anthranilamide compounds were designed by utilizing structure-based design strategies. Optimization at P1 and P4 groups led to the discovery of compound 16g: a highly potent, selective fXa inhibitor with pronounced in vitro anticoagulant activity. Moreover, 16g also displayed excellent in vivo antithrombotic activity in the rat venous thrombosis (VT) and arteriovenous shunt (AV-SHUNT) models. The bleeding risk evaluation showed that 16g had a safer profile than that of betrixaban at 1 mg/kg and 5 mg/kg dose. Additionally, 16g also exhibited satisfactory PK profiles. Eventually, 16g was selected to investigate its effect on hypoxia-reoxygenation- induced H9C2 cell viability. MTT results showed that H9C2 cell viability can be remarkably alleviated by 16g.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP88686	Anthranilamide		88-68-6	Price

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