Article
Evaluation of retro-inverso modifications of HTLV-1 protease inhibitors containing a hydroxyethylamine isoster.
Bioorganic & medicinal chemistry - 1 Apr 2010
Tatsumi Tadashi, Awahara Chiyuki, Naka Hiromi, Aimoto Saburo, Konno Hiroyuki, Nosaka Kazuto, Akaji Kenichi
Abstract excerpt
Effects of retro-inverso (RI) modifications of HTLV-1 protease inhibitors containing a hydroxyethylamine isoster backbone were clarified. Construction of the isoster backbone was achieved by a stereoselective aldol reaction. Four diastereomers with different configurations at the isoster hydroxyl site and the scissile site substituent were synthesized. Inhibitory activities of the new inhibitors suggest that...
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