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Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2/P3 moieties.

Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2/P3 moieties.

Authors :
Ami E
Nakahara K
Sato A
Nguyen JT
Hidaka K
Hamada Y
Nakatani S
Kimura T
Hayashi Y
Kiso Y
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Aug 01; Vol. 17 (15), pp. 4213-7. Date of Electronic Publication: 2007 May 17.
Publication Year :
2007

Abstract

We designed several HIV protease inhibitors with various d-cysteine derivatives as P(2)/P(3) 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.

Details

Language :
English
ISSN :
0960-894X
Volume :
17
Issue :
15
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
17537628
Full Text :
https://doi.org/10.1016/j.bmcl.2007.05.039