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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.
- 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.
- Subjects :
- Amides chemistry
Cell Line
HIV drug effects
HIV Protease Inhibitors chemistry
Humans
Models, Molecular
Phenylbutyrates chemistry
Thiazoles chemistry
Amides chemical synthesis
Amides pharmacology
Cysteine chemistry
HIV Protease Inhibitors chemical synthesis
HIV Protease Inhibitors pharmacology
Phenylbutyrates chemical synthesis
Phenylbutyrates pharmacology
Thiazoles chemical synthesis
Thiazoles pharmacology
Subjects
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