Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites

JS Kaltenbronn, JP Hudspeth, EA Lunney…

文献索引：Kaltenbronn; Hudspeth; Lunney; Michniewicz; Nicolaides; Repine; Roark; Stier; Tinney; Woo; Essenburg Journal of Medicinal Chemistry, 1990 ,  vol. 33,  # 2  p. 838 - 845

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被引用次数: 74

摘要

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, 3 [CHOHCH2], and had ICM values of 61 and 22 nM, respectively.