Autor: |
Larry J. Markoski, Stephen J. Gracheck, Carolyn Nouhan, Peter J. Tummino, Steven VanderRoest, James Saunders, J. V. N. Vara Prasad, Krishna R. Iyer, Christopher Gajda, Fred E. Boyer, Donna Ferguson, Elizabeth A. Lunney, John M. Domagala, Bradley Dean Tait, Michael Sinz, Donald Hupe, Tod P. Holler, Susan Elizabeth Hagen, Edmund L. Ellsworth |
Rok vydání: |
1999 |
Předmět: |
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Zdroj: |
Bioorganic & Medicinal Chemistry Letters. 9:2217-2222 |
ISSN: |
0960-894X |
Popis: |
Dihydropyran-2-one possessing a sulfamate moiety at the 4-position of the thiophenyl ring were designed to reach S 3 ′ pocket of the HIV protease. Synthetic routes for the preparation of thiotosylates possessing 3-(2- t -butyl-5-methyl-4-sulfamate) phenylthio moiety were established. SAR of various sulfamate analogs including HIV protease binding affinities, antiviral activities and therapeutic indices will be described. |
Databáze: |
OpenAIRE |
Externí odkaz: |
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