Table 2.
Dissociation Constants Determined by Spectral Titration of C. albicans and A. fumigatus CYP51 with VNI, Compounds 1, 2, 3, 11, and 15, Posaconazole, and Voriconazole
| cmpds | C. albicans Kd, nM | fold enhancement (Kd VNI/Kdna) | A. fumigatus Kd, nM | fold enhancement (Kd VNI/Kdn) |
|---|---|---|---|---|
| VNI | 290 ± 27 | 203 ± 10 | ||
| 1 | 13 ± 1 | 22 | 57 ± 6 | 4 |
| 2 | 13 ± 1 | 22 | 55 ± 3 | 4 |
| 3 | 10 ± 6 | 29 | 20 ± 4 | 10 |
| 11 | 25 ± 5 | 12 | 61 ± 3 | 3 |
| 15 | 95 ± 11 | 3 | 132 ± 2 | 1.5 |
| posaconazole | 81 ± 16 | 3.5 | 131 ± 11 | 1.5 |
| voriconazole | 165 ± 9 | 1.8 | 56 ±4 | 3.6 |
a
n, compound number.