Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2/P3 moieties.
Basic Information
ID: ALA1145381
Journal: Bioorg Med Chem Lett
Title: 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.
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.
CiteXplore: 17537628
DOI: 10.1016/j.bmcl.2007.05.039
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