Table 4.
In vitro antifungal activity of tricyclic guanidine derivatives
| Compd No. |
Candida albicans | Candida glabrata | Candida krusei | Cryptococcus neoformans | Aspergillus fumigatus | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
| |||||||||||||||
| IC50 μM |
MIC μM |
MFC μM |
IC50 μM |
MIC μM |
MFC μM |
IC50 μM |
MIC μM |
MFC μM |
IC50 μM |
MIC μM |
MFC μM |
IC50 μM |
MIC μM |
MFC μM |
|
| 12b | 18 | 60 | 60 | - | - | - | 19.76 | 60 | 60 | 8.73 | 15 | 30 | 33.54 | - | - |
| 12c | 3.02 | 5.99 | 5.99 | 2.18 | 2.99 | 2.99 | 2.47 | 2.99 | 2.99 | 2.11 | 2.99 | 2.99 | 5.46 | 11.99 | 11.99 |
| 12f | - | - | - | - | - | - | 33.22 | - | - | 29.54 | 60.79 | 30.39 | - | - | - |
| 12h | - | - | - | - | - | - | 35.89 | 45.35 | 45.35 | 6.71 | 11.33 | 11.33 | - | - | - |
| 12j | - | - | - | - | - | - | - | - | - | 23.71 | 48.9 | 48.9 | - | - | - |
| 12l | - | - | - | - | - | - | 39.21 | - | - | 28.68 | 32.78 | 32.78 | - | - | - |
| 14b | 7.03 | 28.81 | 57.63 | 35.96 | - | - | 13.91 | 28.81 | 28.81 | 4.20 | 3.60 | 3.60 | 35.64 | - | - |
| 14c | 3.89 | 5.80 | 5.80 | 3.75 | 5.80 | 5.80 | 1.87 | 2.90 | 2.90 | 2.39 | 5.80 | 2.90 | 10.11 | 23.20 | 23.20 |
| 14f | 16.44 | 29.15 | 58.30 | 34.66 | 58.30 | - | 11.39 | 29.15 | 29.15 | 12.47 | 14.57 | 14.57 | 35.27 | - | - |
| 14h | 34.93 | - | - | - | - | - | 12.34 | 21.93 | 43.86 | 0.46 | 0.68 | 0.68 | - | - | - |
| 14i | 25.90 | 48.19 | - | - | - | - | 16.84 | 24.09 | 24.09 | 1.03 | 1.51 | 1.51 | 47.78 | - | - |
| 14l | 9.09 | 31.34 | 62.69 | 34.16 | 62.69 | 62.69 | 12.94 | 31.34 | 31.34 | 4.29 | 7.83 | 7.83 | 59.34 | - | - |
| 17b | 22.09 | 38.0 | 76 | - | - | - | 24.37 | 76 | 38 | 17.60 | 38 | 38 | 47.37 | - | - |
| 17c | - | - | - | 17.32 | 32.68 | 65.36 | 9.57 | 16.34 | 16.34 | 2.61 | 8.17 | 8.17 | - | - | - |
| 17h | - | - | - | - | - | - | - | - | - | 16.49 | 31.54 | 31.54 | - | - | - |
| 17j | - | - | - | - | - | - | - | - | - | 35.49 | 66.22 | 66.22 | - | - | - |
| 17l | - | - | - | - | - | - | - | - | - | 76.18 | - | - | - | - | - |
| 20a | - | - | - | - | - | - | - | - | - | 19.96 | 40.16 | 40.16 | - | - | - |
| 20b | - | - | - | - | - | - | - | - | - | 15.34 | 18.0 | 18.0 | - | - | - |
| 20c | - | - | - | 19.0 | 31.34 | 62.69 | 6.99 | 15.67 | 15.67 | 3.66 | 7.83 | 15.67 | - | - | - |
| 20h | - | - | - | - | - | - | - | - | - | 3.56 | 7.55 | 7.55 | - | - | - |
| 20l | 16.79 | 31.74 | 31.74 | 19.30 | 31.74 | 63.49 | 8.98 | 15.87 | 15.87 | 2.12 | 3.96 | 3.96 | 34.25 | - | - |
IC50 = Concentration (μM) that affords 50% growth inhibition; MIC= minimum inhibitory concentration (the lowest concentration in μM that allows no detectable growth); MFC = minimum fungicidal concentration (the lowest concentration in μM that kills the organism); “-” = No activity at the highest test concentration of 20 μg/mL. Amphotericin B: IC50 = 0.30 μM, MIC = 1.35 μM, MFC = 1.35 μM (Ca); IC50 = 0.39 μM, MIC = 0.68 μM, MFC = 1.35 μM (Cg); IC50 = 0.56 μM, MIC = 1.35 μM, MFC = 1.35 μM (Ck); IC50 = 0.86 μM, MIC = 1.35 μM, MFC = 2.57 μM (Afu); IC50 = 0.26 μM, MIC = 0.68 μM, MFC = 0.68 μML (Cn).