Literature DB >> 20226680

Evaluation of retro-inverso modifications of HTLV-1 protease inhibitors containing a hydroxyethylamine isoster.

Tadashi Tatsumi1, Chiyuki Awahara, Hiromi Naka, Saburo Aimoto, Hiroyuki Konno, Kazuto Nosaka, Kenichi Akaji.   

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. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20226680     DOI: 10.1016/j.bmc.2010.02.019

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  1 in total

1.  The Effects of Side-Chain Configurations of a Retro-Inverso-Type Inhibitor on the Human T-Cell Leukemia Virus (HTLV)-1 Protease.

Authors:  Chiyuki Awahara; Daiki Oku; Saki Furuta; Kazuya Kobayashi; Kenta Teruya; Kenichi Akaji; Yasunao Hattori
Journal:  Molecules       Date:  2022-03-02       Impact factor: 4.411

  1 in total

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