TABLE 2.
IC50s for inhibitors at three exposure times as determined by the reduction in cellular ATP contents of P. carinii f. sp. carinii populations
| Drug | IC50 (μg/ml [μM]) at the
following treatment time (h):
|
||
|---|---|---|---|
| 24 | 48 | 72 | |
| HMG-CoA reductase inhibitors | |||
| Simvastatin | —a | — | 101.39 (2,422) |
| Lovastatin | — | — | — |
| L-647,318 | — | — | — |
| L-654,164 | — | — | — |
| Squalene synthase inhibitors | |||
| CCI 14993 | 1,244.51 (2,832) | 7.89 (18) | 3.91 (8) |
| CCI 16543 | 138.68 (434) | 21.83 (68) | 10.45 (33) |
| Squalestatin (GR 105155X) | — | — | — |
| Squalene epoxidase inhibitors | |||
| Terbinafine | 1,706.08 (5,863) | 36.98 (130) | 3.67 (13) |
| Tolnaftate | — | 1,221.80 (3,980) | 49.90 (1,625) |
| Squalene epoxide-lanosterol cyclase inhibitors | |||
| GR 90525A | 1.89 (7) | 1.06 (4) | 0.93 (3) |
| GR 193018A | 8.07 (30) | 2.82 (11) | 2.23 (8) |
| GR 54985A | 40.27 (121) | 5.44 (16) | 2.85 (9) |
| UI 8666A | 30.76 (212) | 8.79 (60) | 9.71 (67) |
| GR 31149A | 1,419.10 (4,464) | 14.80 (47) | 1.90 (6) |
| Lanosterol demethylase inhibitors | |||
| GR 40317A | 12.33 (33) | 2.90 (8) | 2.02 (5) |
| GR 42539X | 23.71 (81) | 2.33 (8) | 1.98 (7) |
| GR 40665X | 194.53 (692) | 127.35 (453) | 104.47 (372) |
| Fluconazole | — | — | — |
| GR 71539X | — | — | — |
| GR 77303X | — | — | — |
| Δ8 to Δ7 isomerase inhibitor, AY 9944 | 25.06 (51) | 17.82 (36) | 3.68 (7) |
| SAM:SMT inhibitors | |||
| 24(25)-Epiminolanosterol | — | 2,084.49 (4,737) | — |
| 24-Bromolanosterol | — | — | — |
| 24-Iodolanosterol | — | — | — |
| Sinefungin | — | — | — |
| Polyene antimycotic, amphotericin B | 1.84 (2) | 1.06 (1) | 0.94 (1) |
a
—, inhibition was always less than 50%.