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Antimicrobial Agents and Chemotherapy, 05 1997, 1058-1063, Vol 41, No. 5
Copyright © 1997 by the American Society for Microbiology. All rights reserved.

Antiviral activity of the dihydropyrone PNU-140690, a new nonpeptidic human immunodeficiency virus protease inhibitor

SM Poppe, DE Slade, KT Chong, RR Hinshaw, PJ Pagano, M Markowitz, DD Ho, H Mo, RR Gorman 3rd, TJ Dueweke, S Thaisrivongs and WG Tarpley
Pharmacia & Upjohn, Inc., Kalamazoo, Michigan 49001, USA.

PNU-140690 is a member of a new class of nonpeptidic human immunodeficiency virus (HIV) protease inhibitors (sulfonamide- containing 5,6-dihydro-4-hydroxy-2-pyrones) discovered by structure- based design. PNU-140690 has excellent potency against a variety of HIV type 1 (HIV-1) laboratory strains and clinical isolates, including those resistant to the reverse transcriptase inhibitors zidovudine or delavirdine. When combined with either zidovudine or delavirdine, PNU- 140690 contributes to synergistic antiviral activity. PNU-140690 is also highly active against HIV-1 variants resistant to peptidomimetic protease inhibitors, underscoring the structural distinctions between PNU-140690 and substrate analog protease inhibitors. PNU-140690 retains good antiviral activity in vitro in the presence of human plasma proteins, and preclinical pharmacokinetic studies revealed good oral bioavailability. Accordingly, PNU-140690 is a candidate for clinical evaluation.


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