Table 1. ABS P. falciparum (Dd2 strain) growth inhibition potencies of 1 and racemic benzo-ring substitution variantsa.
| ||
|---|---|---|
| Compound | X | Dd2 strain P. falciparum growth inhibition EC50 (nM) |
| 1 | H | 250 ± 70 nMb |
| (±)-16a | 5-Me | >10 000 nM |
| (±)-16b | 6-Me | >10 000 nM |
| (±)-16c | 7-Me | >10 000 nM |
| (±)-16d | 8-Me | >10 000 nM |
| (±)-17a | 5-CF3 | >10 000 nM |
| (±)-17c | 7-CF3 | 1250–2500 nM |
| (±)-18b | 6-Br | >10 000 nM |
| (±)-19a | 5-Cl | >10 000 nM |
Growth inhibition (EC50 values) of ABS was determined using SYBR Green I assay at 72 h endpoint. P. falciparum Dd2 strain is multi-drug resistant.
Previously reported.8