TABLE 2.
Activity of benzoxaborole compounds against intracellular Leishmania amastigotesa
| Compound | n | EC50 (95% CI) (μM) |
||||
|---|---|---|---|---|---|---|
| L. tropica | L. major | L. aethiopica | L. mexicana | L. panamensis | ||
| Amphotericin B | 1 | 0.066 (0.062–0.070) | 0.043 (0.037–0.049) | 0.115 (0.107–0.122) | 0.430 (0.394–0.460) | 0.143 (0.131–0.156) |
| 2 | 0.083 (0.078–0.089) | 0.049 (0.043–0.056) | 0.107 (0.096–0.119) | 0.685 (0.553–0.692) | 0.115 (0.093–0.142) | |
| Miltefosine | 1 | 19.99 (17.40–22.97) | 44.85 (22.02–77.28) | 7.79 (6.20–9.78) | 31.04 (28.56–33.73) | 19.98 (16.17–24.69) |
| 2 | 9.44 (7.78–11.45) | 26.58 (21.30–33.15) | 7.95 (7.26–8.69) | 45.86 (36.61–57.45) | 23.11 (20.41–26.18) | |
| LSH001 | 1 | 2.01 (1.52–2.67) | 4.26 (2.97–6.11) | 22.10 (15.07–32.41) | 23.04 (15.99–33.19) | 18.82 (14.08–25.14) |
| 2 | 3.12 (2.38–4.09) | 7.61 (5.48–10.57) | 26.83 (19.40–37.11) | 16.94 (9.62–29.83) | 13.96 (10.06–19.44) | |
| LSH002 | 1 | 14.96 (11.38–19.67) | 16.52 (11.56–23.61) | >30 | >30 | >30 |
| LSH003 | 1 | 2.46 (1.78–3.41) | 3.93 (3.32–4.64) | 11.12 (7.67–16.13) | 18.94 (10.78–33.29) | 8.09 (6.56–9.96) |
| 2 | 3.94 (2.96–5.25) | 3.10 (2.25–4.26) | >30 | >30 | 19.05 (15.03–24.16) | |
| LSH004 | 1 | 16.08 (13.70–18.80) | 29.97 (19.04–47.16) | >30 | >30 | |
| LSH005 | 1 | 6.81 (5.84–7.94) | 21.25 (13.18–34.26) | >30 | >30 | |
| LSH006 | 1 | >30 | 25.36 (15.88–40.50) | >30 | >30 | |
| LSH007 | 1 | 5.71 (4.39–7.43) | 27.18 (17.16–43.04) | >30 | >30 | |
| LSH008 | 1 | >30 | >30 | >30 | >30 | |
| LSH009 | 1 | 3.08 (2.51–3.79) | 17.66 (12.10–25.76) | >30 | >30 | |
| LSH010 | 1 | 6.23 (5.49–7.06) | >30 | 11.71 (7.22–19.00) | >30 | >30 |
| LSH011 | 1 | 2.31 (1.73–3.08) | 9.92 (8.49–11.59) | >30 | >30 | >30 |
| LSH012 | 1 | 24.61 (14.31–42.30) | 9.52 (6.80–13.32) | >30 | >30 | >30 |
| LSH013 | 1 | >30b | >30 | >30 | >30 | >30 |
| LSH014 | 1 | 5.91b (4.63–7.54) | 4.15 (3.42–5.04) | >30 | >30 | 29.59 (20.59–42.53) |
| LSH015 | 1 | 6.92 (4.95–9.66) | >30 | >30 | >30 | >30 |
| LSH016 | 1 | 5.40 (4.02–7.26) | >30 | 21.84 (14.60–32.66) | >30 | >30 |
| LSH017 | 1 | >30 | >30 | >30 | >30 | >30 |
| LSH018 | 1 | >30 | >30 | >30 | >30 | >30 |
| LSH019 | 1 | 21.01 (4.07–108.4) | >30 | >30 | >30 | >30 |
| LSH020 | 1 | >30 | >30 | >30 | >30 | >30 |
| LSH021 | 1 | 28.81 (17.03–48.74) | >30 | >30 | >30 | >30 |
| LSH022 | 1 | >30 | >30 | >30 | >30 | >30 |
| LSH023 | 1 | 1.19b (0.78–1.80) | 1.57 (1.17–2.10) | 23.05 (10.09–52.62) | 6.31 (4.18–9.54) | 2.98 (2.28–3.90) |
| LSH024 | 1 | 4.72b (3.31–6.74) | 13.96 (11.52–16.91) | >30 | >30 | 22.34 (17.66–28.25) |
| LSH025 | 1 | 2.21b (1.51–3.25) | 5.93 (5.08–6.92) | >30 | 25.39 (15.81–40.78) | 15.85 (12.85–19.56) |
a
n, number of experiment repeats; CI, confidence interval.
b
L. tropica HTD4 instead of L. tropica AO21/p.