Figure 1.

Examples of the previous series of tertiary alcohol-containing HIV-1 PIs. Spacers are indicated in red: A, one-carbon spacer (K_i = 5.5 nM);²³⁻²⁵B, two-carbon spacer (K_i = 2.3 nM);²⁶C, three-carbon spacer (K_i = 2.8 nM);²⁷D, novel lactam-based inhibitors with two-carbon spacer (K_i = 0.8 nM) and altered stereocenters indicated by asterisks; E, three-carbon spacer (K_i = 4.2 nM). ATZ is included for comparison (K_i = 2.7 nM).³⁷