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

ACS medicinal chemistry letters(2017)

Cited 4|Views31
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Abstract
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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Key words
FVIIa,anticoagulant,antithrombotic,factor VIIa,macrocycle,thrombosis
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