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

Susan M. Poppe | Zendy; Dea Slade | Zendy; K. T. Chong | Zendy; Roger R. Hinshaw | Zendy; P J Pagano | Zendy; Martin Markowitz | Zendy; David D. Ho | Zendy; Hongmei Mo | Zendy; Robert R. Gorman | Zendy; T J Dueweke | Zendy; Suvit Thaisrivongs | Zendy; W. Gary Tarpley | Zendy

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

Author(s) -

Susan M. Poppe,

Dea Slade,

K. T. Chong,

Roger R. Hinshaw,

P J Pagano,

Martin Markowitz,

David D. Ho,

Hongmei Mo,

Robert R. Gorman,

T J Dueweke,

Suvit Thaisrivongs,

W. Gary Tarpley

Publication year - 1997

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.41.5.1058

Subject(s) - zidovudine , protease , peptidomimetic , virology , potency , protease inhibitor (pharmacology) , pharmacology , reverse transcriptase , virus , biology , in vitro , enzyme , biochemistry , viral disease , viral load , peptide , rna , antiretroviral therapy , gene

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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