Table 2.

Enzyme inhibitory and antiviral activity of inhibitors 14a-h and 15a-h

Ring size	Inhibitor structure	Ki(nM)	IC50(nM)a
15		0.38 ± 0.03	120
15		0.82 ± 0.03	318
14		0.082 ± 0.008	4
14		0.67 ± 0.02	49
13		0.0045 ± 0.005	2
13		0.47 ± 0.002	22
12		0.058 ± 0.005	14
12		0.017 ± 0.001	14
12		0.08 ± 0.02	23
11		0.077 ± 0.004	20
11		0.15 ± 0.01	95
10		0.051 ± 0.004	15
10		0.09 ± 0.01	5.5
9		2.4 ± 0.3	n.t.b
9		1.27 ± 0.03	77

^aMT-2 human T-lymphoid cells exposed to HIV-1_LAI; Saquinavir and amprenavir exhibited IC₅₀ values of 16 nM and 27 nM, respectively.

^bn.t. = not tested.