Antiviral activity of UIC-PI, a novel inhibitor of the human immunodeficiency virus type 1 protease

ORCiD

Nejat Düzgüneş: 0000-0001-6159-1391

Department

Biomedical Sciences

Document Type

Article

Publication Title

Antiviral Research

ISSN

0166-3542

Volume

54

Issue

1

DOI

10.1016/S0166-3542(01)00209-1

First Page

29

Last Page

36

Publication Date

3-23-2002

Abstract

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.

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