TABLE 2.
Characteristics of the eight compounds showing antitoxoplasmic activity according to our hit criteria with pyrimethamine as reference drugf
| Anti-Toxoplasma gondii compounda | Mol wtb | cLogPb | IC50c (μM) | CC50d (μM) | SIe |
|---|---|---|---|---|---|
| MMV675968 | 359.81 | 2.31 | 0.02 ± 0.002* | 5.5 | 275 |
| MMV689480 | 326.43 | 4.69 | 0.10 ± 0.049* | 8.66 | 86.6 |
| MMV687807 | 383.67 | 2.63 | 0.15 ± 0.021* | 1.69 | 11.3 |
| MMV022478 | 545.93 | 2.55 | 0.29 ± 0.021* | 2.23 | 7.7 |
| MMV011765 | 358.73 | 3.10 | 0.34 ± 0.007* | 9.48 | 27.9 |
| MMV676602 | 460.57 | 2.09 | 0.81 ± 0.099* | 3.30 | 4.1 |
| MMV676512 | 347.39 | 2.95 | 0.86 ± 0.113* | 3.61 | 4.2 |
| MMV021013 | 294.40 | 3.55 | 1.12 ± 0.035 | 15.92 | 14.2 |
| PYR | 248.71 | 3.00 | 1.17 ± 0.076 | 10.52 | 9.0 |
Compounds are named by their MMV identifier codes. PYR, pyrimethamine.
Molecular weight and cLogP values were obtained from Pathogen Box supporting information, except for pyrimethamine, for which data were found on http://DrugCentral.org.
Compounds were diluted by a 2-fold dilution series and tested in cell culture. Results are means from four values from two different experiments. *, P < 0.05 compared to values for PYR.
Cytotoxicity against Vero cells was evaluated in cell culture. Results are means from four values from two different experiments.
Selectivity indexes were calculated based on the CC50 Vero cells/IC50 T. gondii ratio.
Hit criteria were an IC50 of <2 μM and SI of >4.