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 Chemjournal_title
Bioorganic & medicinal chemistryauthors
Awahara C,Tatsumi T,Furuta S,Shinjoh G,Konno H,Nosaka K,Kobayashi K,Hattori Y,Akaji Kdoi
10.1016/j.bmc.2014.02.050subject
Has Abstractpub_date
2014-04-15 00:00:00pages
2482-8issue
8eissn
0968-0896issn
1464-3391pii
S0968-0896(14)00156-4journal_volume
22pub_type
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