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- W2031562893 abstract "The nonpeptide compounds C1 (4-hydroxy-3-(3-phenoxypropyl)-1-benzopyran-2-one) and P1 (4-hydroxy-6-phenyl-3-(phenylthio)-pyran-2-one) are structurally novel low micromolar inhibitors of the protease of human immunodeficiency virus type 1 (HIV-1). Kinetic analysis revealed that both compounds are competitive inhibitors, with Ki values of 1.0 μM (C1) and 1.1 μM (P1), that act in a reversible fast-binding manner. Structural analogs of both compounds indicate that the pyran-2-one group, the 4-hydroxyl group and substitution at the 3 position are all necessary for inhibitory activity. These two pyranones provide execellent initial compounds in the development of therapeutically effective HIV-1 protease inhibitors, since they are small achiral nonpeptide molecules more easily synthesized and with potentially better pharmacological characteristics than peptide inhibitors of the protease." @default.
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- W2031562893 date "1994-05-01" @default.
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- W2031562893 title "Competitive Inhibition of HIV-1 Protease by 4-Hydroxy-benzopyran-2-ones and by 4-Hydroxy-6-phenylpyran-2-ones" @default.
- W2031562893 doi "https://doi.org/10.1006/bbrc.1994.1642" @default.
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