Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands.

Article Details

Citation

Chen X, Kempf DJ, Sham HL, Green BE, Molla A, Korneyeva M, Vasavanonda S, Wideburg NE, Saldivar A, Marsh KC, McDonald E, Norbeck DW

Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands.

Bioorg Med Chem Lett. 1998 Dec 15;8(24):3531-6.

PubMed ID
9934466 [ View in PubMed
]
Abstract

The 2-isopropyl thiazolyl group is a highly optimized P3 ligand for C2 symmetry-based HIV protease inhibitors, as exemplified in the drug ritonavir. Here we report that incorporation of this P3 ligand into a piperazine hydroxyethylamine series also yielded novel, highly potent inhibitors. In tissue culture assays, the presence of human serum was less deleterious to the activity of these inhibitors than to that of ritonavir. Furthermore, potent activity against ritonavir resistant HIV was observed.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RitonavirCytochrome P450 3A4IC 50 (nM)250N/AN/ADetails