Table 1. In VitroP. falciparum Growth Inhibition of 1a, 13e Stereoisomers, and 7e·HCl.
Compound | EC50 (nM)a | IPP rescueb |
---|---|---|
1a | 250 ± 70c | 100% @ 2.5 μM |
(1R,3S)-(−)-13e | 1,950 ± 240 | 50% @ 5 μM |
(1S,3S)-(−)-13e | 1,300 ± 100 | nd |
(1S,3R)-(+)-13e | 3,690 ± 310 | nd |
(1R,3R)-(+)-13e | 1,430 ± 70 | nd |
7e·HCl | 108 ± 7 | 0% @ 2.5 μM |
Growth inhibition (72 h) of asexual blood stages determined using SYBR Green I assay. Values represent average ± SEM from at least three independent biological replicates. The Dd2 strain is resistant to chloroquine, pyrimethamine, and mefloquine.
Recovery of parasite growth in the presence of 200 μM IPP, at the indicated concentration of the test compound (Supporting Information); nd designates “not determined”.
Reported previously.8