Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines.

Austin Chen,Renee Aspiotis,Louis-Charles Campeau,Elizabeth Cauchon,Amadine Chefson,Yves Ducharme,Jean-Pierre Falgueyret,Sébastien Gagné,Yongxin Han,Robert Houle,Sébastien Laliberté,Guillaume Larouche,Jean-François Lévesque,Dan McKay,David Percival

Bioorganic & Medicinal Chemistry Letters（2012）

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摘要

By restricting the starting scaffold to its bioactive conformation in the renin enzyme, concomitant improvements in both renin potency and off-target profile (i.e., hERG and CYP) were realized.

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关键词

Renin,Inhibitor,Hypertension,CYP,hERG,Spirocyclization

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