Table 1.
The Inhibition of human AspH by regioisomers and C‐3 derivatives of 2,4‐PDCA.
|
|
Compound |
IC50 [μM][a] |
|---|---|---|
|
1 |
2,4‐PDCA (1) |
0.03 ±0.01 |
|
2 |
2,3‐PDCA (5) |
0.51 ±0.05 |
|
3 |
2,5‐PDCA (6) |
inactive |
|
4 |
2,6‐PDCA (7) |
5.48 ±0.75 |
|
5 |
8 |
38.8 ±7.0 |
|
6 |
9 |
inactive |
|
7 |
10 |
inactive |
|
8 |
11 |
10.4 ±1.8 |
|
9 |
12 |
16.1 ±4.0 |
|
10 |
13 |
22.1 ±1.5 |
|
11 |
14 |
12.9 ±1.5 |
|
12 |
15 |
13.8 ±0.2 |
|
13 |
16 |
16.1 ±2.5 |
|
14 |
17 |
4.67 ±0.29 |
|
15 |
18 |
0.58 ±0.06 |
[a] Mean average of two independent runs (n=2; mean ± standard deviation, SD). AspH inhibition assays were performed as described in the Experimental Section using 50 nM His6‐AspH315‐758 and 1.0 μM hFX‐CP101‐119 (Figure 2D) as a substrate.