Antiviral activity of UIC-PI, a novel inhibitor of the human immunodeficiency virus type 1 protease
Nejat Düzgüneş: 0000-0001-6159-1391
The human immunodeficiency virus type 1 (HIV-1) protease inhibitor UIC-PI (1) was developed via structure-based design and incorporated a novel bis-tetrahydrofuran (bis-THF) ligand in the (R)-(hydroxyethyl)sulfonamide based isostere. The EC50 and EC90 of the compound in acutely-infected H9 cells were <1 and ∼1 nM, respectively. In chronically infected H9/HIV-1IIIB cells, the EC50 and EC90 were 20 and 50 nM, respectively. In parallel studies comparing UIC-PI and saquinavir in H9/HIV-1IIIB cells, viral p24 levels in culture supernatants were an order of magnitude lower with UIC-PI than with saquinavir. © 2002 Elsevier Science B.V. All rights resrved.
Ghosh, A. K.,
Antiviral activity of UIC-PI, a novel inhibitor of the human immunodeficiency virus type 1 protease.
Antiviral Research, 54(1), 29–36.