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Inhibitors of HIV protease: Unique non-peptide active site templates

✍ Scribed by Bradley D. Tait; John Domagala; Edmund L. Ellsworth; Donna Ferguson; Christopher Gajda; Donald Hupe; Elizabeth A. Lunney; Peter J. Tummino

Publisher: John Wiley and Sons
Year: 1996
Tongue: English
Weight: 405 KB
Volume: 9
Category: Article
ISSN: 0952-3499
DOI: 10.1002/(sici)1099-1352(199603)9:2<139::aid-jmr249>3.0.co;2-h

No coin nor oath required. For personal study only.

✦ Synopsis

New templates were designed and prepared which straddle the active site of HIV-1 protease. These templates were designed to be 'flexible scaffolds' upon which substituents could be appended to fill the pockets of HIV protease. The new templates prepared and analysed were 4-hydroxy-5H-furan-2-ones, 4-hydroxy-5,6-dihydropyrones, 3-hydroxy-cyclohex-2-enones, and 4-hydroxy-2(lH)-pyridinones, of which the 4-hydroxy-5,6-dihydropyrones were found to be the most potent inhibitors of HIV-1 protease.

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