TABLE 2.
Compound | Y1 | Y2a | R1 | R2 |
C. albicans
|
C. neoformans
|
||
---|---|---|---|---|---|---|---|---|
MIC (μg/ml) | MFC (μg/ml) | MIC (μg/ml) | MFC (μg/ml) | |||||
Amphotericin B | 1.0b | NTc | 1.0b | NT | ||||
Fluconazole | 0.25 | NAd | 2.0 | NA | ||||
16 | NH | NH2 | H | H | 6.25 | 25 | 12.5 | 25 |
17 | NH | NH2 | CH3 | CH3 | 6.25 | 6.25 | 3.12 | 3.12 |
18 | NOCH3 | NH2 | H | H | >100 | NT | >100 | NT |
19 | NH | NH-cPr | H | H | 25 | 25 | 3.12 | 50 |
20 | NH | NH-cBt | H | H | 6.25 | >50 | 0.78 | 6.25 |
21 | NH | NH-cPt | H | H | 6.25 | 25 | 0.78 | 6.25 |
22 | NH | NH-cHx | H | H | 12.5 | 12.5 | 1.56 | 6.25 |
23 | NH | NH-CH2-cPr | H | H | 6.25 | 25 | 0.78 | 6.25 |
24 | NH | NH-CH2)2CH3 | H | H | 12.5 | 12.5 | 1.56 | 6.25 |
25 | NH | NH-CH(CH3)2 | H | H | 25 | 50 | 6.25 | 50 |
26 | NH | NH-CH(CH2CH3)2 | H | H | 100 | 100 | 12.5 | 12.5 |
27 | NH | NH-CH2-CH(CH3)2 | H | H | 12.5 | NT | 3.12 | 12.5 |
28 | NH | NH-(CH2)2-CH(CH3)2 | H | H | 12.5 | 12.5 | 6.25 | 12.5 |
29 | NH | NH-(CH2)3-Pyr | H | H | 100 | NT | 6.25 | 25 |
30 | NH | NH-(CH2)3PipCH3 | H | H | >100 | NT | 12.5 | 50 |
31 | NH | NH-(CH2)4-NH(CH3)2 | H | H | 12.5 | 25 | ≤0.09 | 0.19 |
32 | NH | NH-(CH2)6-NH(CH3)2 | H | H | >100 | NT | 1.56 | 3.12 |
33 | ONH-(CH2)3Oxz | H | H | >100 | NT | >100 | NT | |
34 | ONH-(CH2)2-NH(CH3)2 | H | H | >100 | NT | >100 | NT | |
35 | ONH-(CH2)3-NH(CH3)2 | H | H | >100 | NT | >100 | NT | |
36 | ONH-(CH2)3-NHCH3Ph | H | H | >100 | NT | >100 | NT | |
37 | ONCH3-(CH2)3-NH(CH3)2 | H | H | >100 | NT | >110 | NT |