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Design and Preparation of Potent, Nonpeptidic, Bioavailable Renin Inhibitors †

✍ Scribed by Bezençon, Olivier; Bur, Daniel; Weller, Thomas; Richard-Bildstein, Sylvia; Remeň, Luboš; Sifferlen, Thierry; Corminboeuf, Olivier; Grisostomi, Corinna; Boss, Christoph; Prade, Lars; Delahaye, Stéphane; Treiber, Alexander; Strickner, Panja; Binkert, Christoph; Hess, Patrick; Steiner, Beat; Fischli, Walter


Book ID
123613054
Publisher
American Chemical Society
Year
2009
Tongue
English
Weight
758 KB
Volume
52
Category
Article
ISSN
0022-2623

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Two types of P1-P3-linked macrocyclic renin inhibitors containing the hydroxyethylene isostere (HE) scaffold just outside the macrocyclic ring have been synthesized. An aromatic or aliphatic substituent (P3sp) was introduced in the macrocyclic ring aiming at the S3 subpocket (S3sp) in order to optim