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Table 3 Wild type CSA HIV-1 protease inhibition activities of PCU-lactam-NH- and lactone-CO-peptides

From: Pentacycloundecane lactam vs lactone norstatine type protease HIV inhibitors: binding energy calculations and DFT study

  Peptide IC 50 with lactam-NH- (μM)* IC 50 with lactone-CO- (μM)*
Mixture of both diastereomers Glu-Ala-Ile-Ser 0.078 ± 0.0035 0.85 ± 0.18
  1. *IC50 = 50% inhibition constant reported as the average of three experiments. Standard deviations (SD) for all compounds were ≤ 2% of the reported IC50 values. Peptides were isolated as a mixture of diastereomers. Atazanavir (IC50 = 0.004 ± 0.00071 μM) and Lopinavir (IC50 = 0.025 ± 0.0014 μM) were used as standards for the testing.