| Autor: |
Sham, H.L., Zhao, C., Marsh, K.C., Betebenner, D.A., Lin, S.Q., Mcdonald, E., Vasavanonda, S., Wideburg, N., Saldivar, A., Robins, T., Kempf, D.J., Plattner, J.J., Norbeck, D.W. |
| Zdroj: |
Biochemical and Biophysical Research Communications; June 1995, Vol. 211 Issue: 1 p159-165, 7p |
| Abstrakt: |
A series of novel pseudo-symmetrical and unsymmetrical inhibitors based on the backbone modification of a peptidomimetic were synthesized and found to be highly potent inhibitors of the HIV-1 protease (IC50= 2.9 to <0.5 nM). These compounds also possess good antiviral activity in vitroas measured by inhibition of the cytopathic effect of HIV-13Bin MT-4 lymphocytes. Importantly, some of these compounds also have good oral bioavailabilities in rats (F=30.6% to 100%). One of these compounds 4C, also has good oral bioavailability in beagle dogs and cynomolgus monkeys. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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