Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites
James S. Kaltenbronn(Warde Medical Laboratory), James P. Hudspeth, E. A. Lunney, Barbara M. Michniewicz, Ernest D. Nicolaides, Joseph T. Repine, W. Howard Roark, Michael A. Stier, Francis J. Tinney
Cited by 74Open Access
Abstract
Renin inhibitors having 13 different isosteres connecting the P3 and P2 positions have been prepared. Synthetic routes and in vitro activity exhibited by these compounds are discussed. The two most potent compounds, 47 and 48, contained the hydroxyethylene isostere, psi [CHOHCH2], and had IC50 values of 61 and 22 nM, respectively.
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