Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369596 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
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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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yuji Nakamura, Chie Sugita, Masaki Meguro, Shojiro Miyazaki, Kazuhiko Tamaki, Mizuki Takahashi, Yoko Nagai, Takahiro Nagayama, Mikio Kato, Hiroshi Suemune, Takahide Nishi,