Table 6.
Potency (μM) Ave. ± S.E.M. | |||||
---|---|---|---|---|---|
Entry | R1 | R2 | Yield % a | PfG6PD Primary Assay | PfG6PD NADPH Kinetic |
28 | 2-F | P | 9.5 ± 3.6 | 11.0 | |
29 | 2-F | 18 | 16.2 ± 2.1 | 25.2 | |
30 | 4-OMe | P | 49.7 ± 13.7 | >80.0 | |
31 | 2-Cl | P | 11.1 ± 1.3 | >80.0 | |
32 | 3-Me | P | 11.8 ± 0.4 | 8.8 | |
33 | 2-F | 6 | 21.6 ± 3.4 | 24.0 | |
34 | 2-F | 15 | >80.0 | >80.0 | |
35 | 2-F | P | 46.6 ± 10.0 | 11.0 | |
36 | 2-Cl | P | 40.9 ± 12.5 | >80.0 | |
37 | 3-OMe | P | >80.0 | 58.5 | |
38 | 4-OMe | P | >80.0 | >80.0 | |
8b | H | P | 9.3 | 22.3 | |
9b | 3-Cl | P | 17.9 | 34.2 | |
39 | 2-F | 27 | 22.7 ± 2.1 | 45.2 | |
40 | 2-F | 36 | 45.0 ± 5.3 | 35.0 | |
41 | 2-F | 36 | >80.0 | >80.0 | |
42 | 2-F | 46 | >80.0 | 67.8 |
P: commercially purchased compounds
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