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Evaluation of retro-inverso modifications of HTLV-1 protease inhibitors containing a hydroxyethylamine isoster |
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| Authors: | Tadashi Tatsumi Chiyuki Awahara Hiromi Naka Saburo Aimoto Hiroyuki Konno Kazuto Nosaka Kenichi Akaji |
| Affiliation: | 1. Department of Medicinal Chemistry, Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Kita-ku, Kyoto 603-8334, Japan;2. Institute for Protein Research, Osaka University, Suita, Osaka 565-0871, Japan |
| Abstract: | 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 partially modified RI inhibitors would interact with HTLV-1 protease in the same manner as the parent hydroxyethylamine inhibitor. |
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