Table 1.
Antifungal activities of the title compounds in vitro (80% minimal inhibitory concentration μg/mL)
| Compound | -R | Candida albicans 14053 | C. albicans 20352 | Candida parapsilosis | Cryptococcus neoformans | Candida glabrata | Aspergillus fumigatus | Trichophyton rubrum | Microsporum gypseum |
|---|---|---|---|---|---|---|---|---|---|
| 1a | 2-F | 2.00000 | 4.0000 | 16.00000 | 2.0 | >64.0 | >64.00 | 32.0000 | 0.50 |
| 1b | 3-F | 0.25000 | 0.5000 | 1.00000 | 0.5 | 64.0 | >64.00 | 1.0000 | 0.25 |
| 1c | 4-F | 0.50000 | 1.0000 | 8.00000 | 4.0 | 64.0 | >64.00 | 16.0000 | 2.00 |
| 1d | 2-Cl | 1.00000 | 0.2500 | 8.00000 | 8.0 | 32.0 | >64.00 | 16.0000 | 0.50 |
| 1e | 3-Cl | 2.00000 | 8.0000 | >64.00000 | 16.0 | >64.0 | >64.00 | 32.0000 | 0.25 |
| 1f | 4-Cl | 16.00000 | 32.0000 | 64.00000 | 8.0 | >64.0 | >64.00 | 64.0000 | 1.00 |
| 1g | 2-Br | 2.00000 | 1.0000 | 8.00000 | 4.0 | 64.0 | >64.00 | 16.0000 | 2.00 |
| 1h | 3-Br | 2.00000 | 4.0000 | 32.00000 | 8.0 | >64.0 | >64.00 | 32.0000 | 0.25 |
| 1i | 4-Br | 4.00000 | 8.0000 | 32.00000 | 8.0 | >64.0 | >64.00 | 64.0000 | 16.00 |
| 1j | 2-CH3 | 32.00000 | >64.0000 | >64.00000 | >64.0 | >64.0 | >64.00 | 64.0000 | 64.00 |
| 1k | 3-CH3 | 1.00000 | 1.0000 | 4.00000 | 1.0 | 4.0 | >64.00 | 8.0000 | 8.00 |
| 1l | 4-CH3 | 1.00000 | 1.0000 | 8.00000 | 2.0 | >64.0 | >64.00 | 32.0000 | 8.00 |
| 1m | 2-CN | 2.00000 | 8.0000 | 32.00000 | 16.0 | >64.0 | >64.00 | 32.0000 | 16.00 |
| 1n | 3-CN | 0.12500 | 0.5000 | 4.00000 | 0.5 | 16.0 | >64.00 | 16.0000 | 1.00 |
| 1o | 4-CN | 8.00000 | 32.0000 | >64.00000 | 4.0 | >64.0 | >64.00 | >64.0000 | 4.00 |
| 1p | 2-NO2 | 0.50000 | 4.0000 | 32.00000 | 8.0 | >64.0 | >64.00 | 64.0000 | 8.00 |
| 1q | 3-NO2 | 2.00000 | 2.0000 | 16.00000 | 8.0 | 64.0 | >64.00 | 32.0000 | 64.00 |
| 1r | 4-NO2 | 0.50000 | 2.0000 | 32.00000 | 4.0 | >64.0 | >64.00 | 32.0000 | 1.00 |
| Fluconazole | – | 1.00000 | 0.5000 | 0.50000 | 2.0 | 2.0 | >64.00 | 4.0000 | 64.00 |
| Itraconazole | – | 0.06250 | 0.0625 | 0.03125 | 2.0 | 0.5 | 2.00 | 0.1250 | 4.00 |
| Voriconazole | – | 0.03125 | 0.0625 | 0.03125 | 2.0 | 0.5 | 0.25 | 0.0625 | 0.25 |