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. 2016 Jun 20;60(7):4391–4393. doi: 10.1128/AAC.02816-15

TABLE 1.

Trypanocidal activity of MPA and its derivatives

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
a

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.

b

Pentamidine 500 ng/ml was used as a 100% inhibition control.

c

HMI-9 medium with 0.25% dimethyl sulfoxide (DMSO) was used as a 0% inhibition control.