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ID: ALA3232830
Journal: Bioorg Med Chem
Title: Effect of prime-site sequence of retro-inverso-modified HTLV-1 protease inhibitor.
Authors: Awahara C, Tatsumi T, Furuta S, Shinjoh G, Konno H, Nosaka K, Kobayashi K, Hattori Y, Akaji K.
Abstract: The effects of additional substituents covering the prime-site of retro-inverso (RI)-modified HTLV-1 protease inhibitors containing a hydroxyethylamine isoster were clarified. Stereo-selective construction of the most potent isoster backbone was achieved by the Evans-aldol reaction. Addition of N-acetylated d-amino acid corresponding to the P2' site gave an RI-modified inhibitor showing superior inhibitory activity to the previous inhibitor. Inhibitory activities of the newly synthesized inhibitors suggest that partially modified RI inhibitors would interact with HTLV-1 protease in the same manner as the parent hydroxyethylamine inhibitor.
CiteXplore: 24680060