TABLE 1.
Schistosoma mansoni worm mortality versus concentration of ether lipid esters of acyclic nucleoside phosphonates
| S. mansoni treatment group | % Worm mortality (no. dead/total exposed) at indicated phosphonate concn (μM) |
EC50 | |||||
|---|---|---|---|---|---|---|---|
| 100 | 75 | 50 | 25 | 12.5 | 5 | ||
| Control | 0 | 0 | 0 | 0 | 0 | 0 | |
| DMSO | 0 | 0 | 0 | 0 | 0 | 0 | |
| Praziquantel | 100 | 100 | 100 | 100 | 100 | 100 | 0.22 |
| HDP-cyclic-(S)-HPMPA | 93.3 (14/15) | 84.6 (11/13) | 78.6 (11/14) | 69.2 (9/13) | 53.8 (7/13) | 50 (8/16) | 5.0 |
| HDP-(S)-HPMPA | 30.8 (4/13) | 28.6 (4/14) | 32.3 (10/31) | 18.8 (3/16) | 12.5 (2/16) | 6.25 (1/16) | >100 |
| ODE-(S)-HPMPA | 47 (7/15) | 33 (5/15) | 40 (6/15) | 25 (4/16) | 12.5 (2/16) | 12.5 (2/16) | >100 |
| ODE-(S)-HPMPG | 33 (5/15) | 36 (5/14) | 20 (3/15) | 15 (2/13) | 7 (1/14) | 13 (2/15) | >100 |
| ODE-HPMP-DAP | 40 (6/15) | 40 (6/15) | 33 (4/12) | 14 (2/14) | 8 (1/12) | 7 (1/14) | >100 |
| HDP-cyclic-CDV | 100 (15/15) | 64 (9/14) | 67 (8/12) | 36 (5/14) | 33 (5/15) | 13 (2/15) | 28.0 |
| (S)-HPMPA | 13 (2/15) | 12.5 (2/16) | 7 (1/14) | 7 (1/14) | 6.25 (1/16) | 6.7 (1/15) | >100 |