Effect of prime-site sequence of retro-inverso-modified HTLV-1 protease inhibitor.

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.

journal_name

Bioorg Med Chem

authors

Awahara C,Tatsumi T,Furuta S,Shinjoh G,Konno H,Nosaka K,Kobayashi K,Hattori Y,Akaji K

doi

10.1016/j.bmc.2014.02.050

subject

Has Abstract

pub_date

2014-04-15 00:00:00

pages

2482-8

issue

8

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(14)00156-4

journal_volume

22

pub_type

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