TABLE 1.
Compound | Inhibition rate (%)a |
||
---|---|---|---|
T. congolense | T. b. brucei | T. evansi | |
1 (MPA) | 99.60 ± 0.38 | 82.99 ± 2.82 | 90.53 ± 1.22 |
2 | 94.46 ± 3.89 | 5.24 ± 13.12 | 14.21 ± 8.64 |
3 | 2.36 ± 8.64 | 7.83 ± 10.35 | 16.66 ± 5.55 |
4 | 98.87 ± 0.78 | 46.13 ± 5.21 | 42.79 ± 4.58 |
5 | 4.65 ± 15.29 | 14.29 ± 34.17 | 32.43 ± 4.88 |
6 | 1.45 ± 10.94 | 22.27 ± 4.81 | 17.11 ± 6.14 |
7 | 4.59 ± 15.12 | 14.50 ± 13.76 | 29.44 ± 10.03 |
8 | 3.59 ± 14.06 | 22.99 ± 12.90 | 19.94 ± 8.44 |
9 | 0.06 ± 8.66 | 9.28 ± 5.15 | 11.99 ± 1.59 |
10 | 3.15 ± 8.43 | 9.03 ± 7.91 | 9.49 ± 6.13 |
11 | 6.51 ± 14.38 | 16.47 ± 6.97 | 12.79 ± 4.49 |
12 | 3.03 ± 12.91 | 11.56 ± 4.17 | 13.61 ± 8.67 |
Pentamidineb | 99.93 ± 0.07 | 99.96 ± 0.06 | 99.94 ± 0.07 |
Controlc | 0.00 ± 1.74 | 0.48 ± 1.58 | −0.24 ± 2.25 |
Trypanocidal activity of MPA (compound 1) and 11 MPA derivatives (see Fig. 1) at a concentration of 1 μM was evaluated for T. congolense IL3000 strain, T. b. brucei GUTat 3.1 strain, and T. evansi Tansui strain. The inhibition rate was calculated from 3 independent experiments and expressed as the mean inhibition rate ± SD.
Pentamidine 500 ng/ml was used as a 100% inhibition control.
HMI-9 medium with 0.25% dimethyl sulfoxide (DMSO) was used as a 0% inhibition control.