Table 1.
Biological Activity of Bispyrrolinone HIV-1 Protease Inhibitors. 50% Inhibitory Concentration (IC50); Cellular 95% Inhibitory Concentration (CIC95)
Inhibitor | N-Terminus | C-Terminus | IC50 (nM) | CIC95 (nM) | C/I |
---|---|---|---|---|---|
L-682,679 | Boc | NH2 | 0.6 | 6,000 | 10,000 |
(−)-38 | Boc | NH2 | 10 | 1,500 | 150 |
(−)-39 | Furanyl Carbamate | NH2 | 1.3 | 800 | 615 |
(−)-40 | Furanyl Carbamate | NH-t-Bu | 3.3 | 800 | 242 |