Table 3.
In vitro antiprotozoal activity of triazole conjugates (37–43)
| Compound | L. donovani promastigotes | L. donovani Axenic amastigotes | L. donovani macrophage internalized amastigote | T. brucei | P. falciparum | |||||
|---|---|---|---|---|---|---|---|---|---|---|
| IC50, μM | IC90, μM | IC50, μM | IC90, μM | IC50, μM | IC90, μM | IC50, μM | IC9, μM | IC50 (D6), μM | IC50 (W2), μM | |
| 37 | NA | NA | 21.796 ± 0.001 | >26.777 | 23.537 ±2.286 | >26.777 | 3.935 ± 0.079 | 4.940 ± 0.092 | NA | NA |
| 38 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 39 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 40 | 14.625 ± 5.757 | >22.766 | 18.281 ± 0.592 | 22.447 ± 0.016 | NA | NA | 2.117 ± 0.147 | 6.766 ± 1.918 | 6.322 ± 0.363 | 7.611 ± 0.838 |
| 41 | NA | NA | NA | NA | NA | NA | 4.741 ± 1.735 | 13.514 ±0.988 | 8.367 ± 3.041 | 6.606 ± 0.732 |
| 42 | 16.445 ± 3.868 | >21.722 | 10.536 ± 0.824 | 18.149 ± 1.651 | 8.321 ± 0.327 | 12.879 ±5.811 | 0.926 ± 0.034 | 1.200 ± 0.026 | 1.909 ± 0.403 | 2.886 ± 0.701 |
| 43 | NA | NA | NA | NA | NA | NA | 7.595 ± 2.119 | 10.468 ± 3.234 | 0.697 ± 0.187 | 0.583 ± 0.140 |
| Amp B | 0.192 | 0.312 | 1.729 | 2.004 | 0.272 ± 0.100 | 0.441 ±0.019 | NT | NT | NT | NT |
| Pent | 2.036 | 3.668 | 15.345 | 16.872 | 6.531 | >16.872 | NT | NT | NT | NT |
| DFMO | NT | NT | NT | NT | NT | NT | 21.299 ±2.013 | 59.175 ±5.748 | NT | NT |
| CQ | NT | NT | NT | NT | NT | NT | NT | NT | 0.052 | 0.46 |
NA: not active; NT: not tested; Amp B = Amphotericin B; Pent = pentamidine; DFMO = difluoromethylornithine; CQ = chloroquine