Design, synthesis and biological evaluation of Piperazinylanthranilamides as potential factor Xa inhibitors

Atul N. Khadse, Hardik H. Savsani,Rupesh V. Chikhale,Rahul B. Ghuge, Dixit R. Prajapati, Goshiya Kureshi,Prashant R. Murumkar,Kirti V. Patel,Sadhana J. Rajput,Mange Ram Yadav

Journal of Molecular Structure（2022）

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摘要

•A series of piperazinylanthranilamide derivatives have been designed and synthesized as potential factor Xa inhibitors.•The synthesized compounds displayed good to moderate potency in in vitro studies.•PT and aPTT prolongation properties, and bleeding risk tendency of the compounds were also determined.•Molecular docking and simulation studies, and ADMET calculations supported the potential of the compounds as antithrombotic agents.

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关键词

Factor Xa,Inhibitors,Anthranilamides,Piperazinylanthranilamides,Prothrombin time,Partial thromboplastin time,anticoagulation,thrombin,prothrombin

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