Table 3.
MIC values for compounds against C. albicans SC5314 and CA14 at 48 hours.
|
Cmpd |
|
|
|
MIC [μg/mL] (μM) |
clogP [a] |
|
|---|---|---|---|---|---|---|
|
|
R1 |
R2 |
X |
SC5314 |
CA14 |
|
|
5 b |
4‐F |
H |
CH |
8 (24.7) |
4 (12.4) |
3.14 |
|
5 c |
4‐Cl |
H |
CH |
8 (23.5) |
4 (11.8) |
3.54 |
|
5 d |
4‐Cl |
Cl |
CH |
0.125 (0.33) |
0.125 (0.33) |
4.1 |
|
5 e |
2,4‐diCl |
H |
CH |
1 (2.67) |
1 (2.67) |
4.1 |
|
5 f |
2,4‐diCl |
Cl |
CH |
<0.03 (<0.07) |
<0.03 (<0.07) |
4.66 |
|
5 g |
4‐CH3 |
H |
CH |
8 (25.1) |
8 (25.1) |
3.47 |
|
5 h |
4‐CF3 |
H |
CH |
4 (10.7) |
4 (10.7) |
3.91 |
|
5 i |
4‐OCH3 |
H |
CH |
8 (23.9) |
8 (23.9) |
2.86 |
|
5 j |
3,4‐diOCH3 |
H |
CH |
>16 (>43.8) |
>16 (>43.8) |
2.73 |
|
5 k |
4‐Cl |
H |
N |
8 (23.5) |
8 (23.5) |
3.05 |
|
7 |
– |
– |
– |
>16 (>36.8) |
>16 (>36.8) |
1.69 |
|
12 a |
H |
– |
– |
4 (8.67) |
4 (8.67) |
2.9 |
|
12 b |
4‐F |
– |
– |
4 (8.34) |
2 (4.17) |
3.06 |
|
12 c |
4‐Cl |
– |
– |
1 (2.02) |
1 (2.02) |
3.46 |
|
12 d |
4‐OCH3 |
– |
– |
8 (16.3) |
4 (8.14) |
2.77 |
|
Fluc |
|
|
|
0.125 (0.41) |
0.125 (0.41) |
0.86 |
[a] clogP was determined using Crippen's fragmentation.29