Article ID Journal Published Year Pages File Type
1369596 Bioorganic & Medicinal Chemistry Letters 2012 6 Pages PDF
Abstract

Introduction of the 2,2-dimethyl-4-phenylpiperazin-5-one scaffold into the P3–P1 portion of the (2S,4S,5S)-5-amino-6-dialkylamino-4-hydroxy-2-isopropylhexanamide backbone dramatically increased the renin inhibitory activity without using the interaction to the S3sp pocket. Compound 31 exhibited >10,000-fold selectivity over other human proteases, and 18.5% oral bioavailability in monkey.

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