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ID: ALA1131402
Journal: Bioorg Med Chem Lett
Title: Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands.
Authors: Chen X, Kempf DJ, Sham HL, Green BE, Molla A, Korneyeva M, Vasavanonda S, Wideburg NE, Saldivar A, Marsh KC, McDonald E, Norbeck DW.
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.
CiteXplore: 9934466