Figures & data
Figure 1. Structures of five representative anti-IFI drugs used clinically.
Figure 2. Structure and antifungal activity of hit 1.
Scheme 1. Reagents and conditions: (a) NH2NH2⋅H2O, THF, r.t., 1h; (b) EtOH, 80 °C.
Table 1. In vitro antifungal activity of the target compounds.
Table 2. In vitro activity of selected compounds against Candida glabrata.
Figure 3. The effect of 5j, 5r, and FLC on C. glabrata biofilm formation in vitro. To evaluate the inhibitory activity of compounds 5j and 5r against biofilm formation in C. glabrata ATCC28226 compared with that of FLC by the XTT reduction assay. FLC, fluconazole.
Figure 4. The in vitro toxicity evaluation of 5j, 5n, 5r, 1, FLC and AmB. The cytotoxic effects of compounds 5j, 5n, 5r and 1, compared to that of FLC on HUVECs viability was assessed by the CCK-8 test. FLC, fluconazole; AmB, amphotericin B.
Figure 5. Haemolytic effect of 5j, 5n, 5r, 1, FLC and AmB against rabbit red blood cells at different indicated concentrations.
Figure 6. (A) The BOILED-Egg model prediction of 1, 5j, 5r and FLC; (B) Bioavailability radar for 1, 5j, 5r and FLC; FLC: fluconazole.
