Increased antiviral activity of HIV protease inhibitors of the difluorostatone type bearing (R)-valinol derivatives as novel c-termini
Autor: | T M Brennan, Celine Tarnus, D. Janowick, A. S. Tyms, S. Baltzer, F. Weber, V. Van Dorsselaer, D.L. Taylor, J.M. Remy, Daniel Schirlin |
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Rok vydání: | 1994 |
Předmět: |
chemistry.chemical_classification
Protease biology Stereochemistry medicine.medical_treatment Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry In vitro Virus chemistry.chemical_compound Enzyme chemistry Enzyme inhibitor Drug Discovery medicine biology.protein Molecular Medicine Cytotoxic T cell HIV Protease Inhibitor Valinol Molecular Biology |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 4:1213-1218 |
ISSN: | 0960-894X |
DOI: | 10.1016/s0960-894x(01)80332-2 |
Popis: | Replacement of the benzylamine carboxy terminus with a (R)-valinol ether carboxy terminus confers high inhibitory activity to derivatives of the difluorostatone and even difluorostatine types against HIV-1 protease. In HIV infected cells, the difluorostatone-containing inhibitor 2 exhibits high antiviral potency and low cytotoxic effects. |
Databáze: | OpenAIRE |
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