Title of article
Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating d-cysteine derivatives as P2/P3 moieties
Author/Authors
Ei’ichi Ami، نويسنده , , Koichiro Nakahara، نويسنده , , Akihiko Sato، نويسنده , , Jeffrey-Tri Nguyen، نويسنده , , Koushi Hidaka، نويسنده , , Yoshio Hamada، نويسنده , , Shingo Nakatani، نويسنده , , Tooru Kimura، نويسنده , , Yoshio Hayashi، نويسنده , , Yoshiaki Kiso، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
4213
To page
4217
Abstract
We designed several HIV protease inhibitors with various d-cysteine derivatives as P2/P3 moieties based on the structure of clinical drug candidate, KNI-764. Herein, we report their synthesis, HIV protease inhibitory activity, HIV IIIB cell inhibitory activity, cellular toxicity, and inhibitory activity against drug-resistant HIV strains. KNI-1931 showed distinct selectivity against HIV proteases and high potency against drug-resistant strains, surpassing those of Ritonavir and Nelfinavir.
Keywords
HIV protease , protease inhibitor , d-Cysteine , Allophenylnorstatine , Drug-resistant HIV strain
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798397
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