Table 1. Effect of P3 sidechain substituents on PfSUB1 inhibitory potency.
Entry | Cmpd. | R1 | IC50, nM PfSUB1 inhibition |
---|---|---|---|
1 | 2a | 2.1±0.1 | |
2 | 2b | 2.8±0.1 | |
3 | 2c | 7.5±0.8 | |
4 | 2d | 6.7±0.3 | |
5 | 2e | 43.5±2.7 | |
6 | 2f | 5.4±0.1 | |
7 | 2g | 7.8±0.1 | |
8 | 2h | 6.9±2.6 |