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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Tatsumi T,Awahara C,Naka H,Aimoto S,Konno H,Nosaka K,Akaji K

doi

10.1016/j.bmc.2010.02.019

subject

Has Abstract

pub_date

2010-04-01 00:00:00

pages

2720-7

issue

7

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(10)00140-9

journal_volume

18

pub_type

杂志文章

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