Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.

Jeremy M Richter,Daniel L Cheney, J Alex Bates,Anzhi Wei,Joseph M Luettgen,Alan R Rendina,Timothy M Harper,Rangaraj Narayanan,Pancras C Wong,Dietmar Seiffert,Ruth R Wexler,E Scott Priestley

ACS medicinal chemistry letters（2017）

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摘要

Two novel series of meta-linked phenylglycine-based macrocyclic FVIIa inhibitors have been designed to improve the rodent metabolic stability and PK observed with the precursor para-linked phenylglycine macrocycles. Through iterative structure-based design and optimization, the TF/FVIIa was improved to subnanomolar levels with good clotting activity, metabolic stability, and permeability.

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关键词

FVIIa,anticoagulant,antithrombotic,factor VIIa,macrocycle,thrombosis

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