Table 1. Antifungal Activities for Phthalazinone and Isoquinolone Analogues Against C. albicans in the Presence of Fluconazolea.
compd | R1 | R2 | EC50 (μM) |
---|---|---|---|
1 | OMe | 0.015 ± 0.002 | |
13 | OMe | H | 0.033 ± 0.005 |
14 | Me | H | 0.065 ± 0.02 |
15 | Br | H | 0.003 ± 0.001 |
16 | C≡C(CH2)3OH | H | >100 |
17 | Br | Br | 0.003 ± 0.001 |
18 | Br | C≡C(CH2)3OH | >100 |
19 | Br | >10 | |
20 | Br | 0.230 ± 0.01 | |
21 | Br | 0.023 ± 0.008 | |
22 | Br | 0.020 ± 0.006 | |
23 | Br | 0.220 ± 0.05 | |
24 | Br | 0.001 ± 0.0003 |
Cells incubated with 0.25 μg/mL fluconazole.