PNU-106893, N-{3-[1-(4-hydroxy-2-oxo-6-phenyl-6-propyl-5,6 -dihydro-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl}-1-methyl-1H-imidazole-4-sulfonamide, is a selective HIV aspartyl protease inhibitor under evaluation as a potential oral treatment of acquired immunodeficiency disease. PNU-106893 is a mixt
Brain Delivery of HIV Protease Inhibitors
β Scribed by Mahmoud M. Sheha; Nawal A. El-Koussi; Hassan H. Farag
- Publisher
- John Wiley and Sons
- Year
- 2003
- Tongue
- English
- Weight
- 85 KB
- Volume
- 336
- Category
- Article
- ISSN
- 0365-6233
No coin nor oath required. For personal study only.
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The interactions of four HIV-protease inhibitors, ritonavir (RIT), saquinavir (SAQ), indinavir (IND) and nelfinavir (NEL), were examined by in vitro metabolic studies using rat liver microsomal fractions. The substrate concentrations employed were 0.75 12 mM, and the inhibitor concentrations were 2.
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