Table 1.
Compound | Activity IC50 (mM)† | Toxicity on Vero cell IC50 (mM)‡ | SI§ | ||
---|---|---|---|---|---|
Epimastigote forms | Axenic amastigote forms | Epimastigote forms | Axenic amastigote forms | ||
Benznidazole | 15.89 ± 1.1 | 18.92 ± 1.1 | 13.60 ± 0.9 | 0.8 | 0.7 |
Compound 1 | 6.10 ± 0.2 | 6.03 ± 0.3 | 98.95 ± 6.2 | 16.2 (20) | 16.4 (23) |
Compound 2 | 7.98 ± 0.8 | 6.81 ± 0.1 | 154.66 ± 17.3 | 19.4 (24) | 22.7 (32) |
Compound 3 | 50.03 ± 6.6 | 30.44 ± 2.3 | 117.67 ± 21.8 | 2.4 (3) | 3.9 (6) |
Compound 4 | 69.01 ± 7.7 | 38.72 ± 3.6 | 163.14 ± 14.5 | 2.4 (3) | 4.2 (6) |
Results are averages of three separate determinations.
IC50 = the concentration required to give 50% inhibition, calculated by linear regression analysis from the Kc values at concentrations used (1, 10, 25, 50, and 100 μM).
On Vero cells after 72 h of culture. IC50 = the concentration required to give 50% inhibition, calculated by linear regression analysis from the Kc values at concentrations used (1, 10, 25, 50 and 100 μM).
Selectivity index = IC50 Vero cells/IC50 epimastigote and axenic amastigote forms of the parasite. In brackets: number of times that compound SI exceeds the reference drug SI.