Table 2.
Rb | Thioether | Sulfoxide | Sulfone | TFDKd | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
N°c | 5 min | 15 min | N° | 5 min | 15 min | N° | 5 min | 15 min | N° | 5 min | 15 min | |
4 | 1 | >40,000 | >40,000 | 6 | >40,000 | >40,000 | N.D.e | N.D. | N.D. | N.D. | ||
6 | 2 | 1950±250 | 2500±190 | 7 | >40,000 | >40,000 | 11 | >40,000 | >40,000 | N.D. | N.D. | |
8 | 3 | 230±20 | 300±30 | 8 | 6500±650 | 13,900±900 | 12 | 14,800±700 | 22,500±1100 | 15 | 1250±110 | 1800±130 |
10 | 4 | 120±10 | 170±20 | 9 | 760±50 | 1350±90 | 13 | 2200±200 | 3000±230 | N.D. | N.D. | |
12 | 5 | 84±7.5 | 89±7.8 | 10 | 440±50 | 600±40 | 14 | 250±10 | 280±30 | N.D. | N.D. |
All values are given as the average ± the standard deviation of 3 replicates in units of nM. Incubation of enzyme and inhibitor was performed for either 5 min or 15 min before addition of substrate as described in the Experimental.
R refers to the number of carbon atoms in the alkyl chain as shown in Figure 1.
Individual compound numbers.
1,1,1-trifluorododecan-2-one.
N.D. indicates that value was not determined.