Table 1 Inhibitory activity of the 4,5-diaryl 2H-1,2,3-triazoles, 4-carboxylate-5-aryl-2H-1,2,3-triazoles and 4-carboxamide-5-aryl-2H-1,2,3-triazoles against purified human IDO1 enzyme.
Substituents | Compound 1 | Compound 2 | Compound 3 | ||||
|---|---|---|---|---|---|---|---|
R1 | R2 | hIDO1 IC50 (µM)a | hIDO1 IC50 (µM)a | hIDO1 IC50 (µM)a | |||
H | H | 1a | 90.033 ± 2.942 | 2a | 14.390 ± 3.357 | 3a | 8.541 ± 0.084 |
H | Me | 1b | 54.871 ± 0.757 | 2b | 1.699 ± 0.061 | 3b | 7.082 ± 0.691 |
F | H | 1c | 4.991 ± 0.057 | 2c | 31.440 ± 4.207 | 3c | 6.611 ± 0.355 |
Cl | H | 1d | 2.513 ± 0.060 | 2d | 2.550 ± 0.033 | 3d | 2.687 ± 0.055 |
Br | H | 1e | 21.870 ± 1.270 | 2e | 2.981 ± 0.012 | 3e | 26.680 ± 2.199 |
H | F | 1f | 25.240 ± 1.703 | 2f | 8.090 ± 0.210 | 3f | 2.941 ± 0.034 |
H | Cl | 1g | 3.208 ± 0.100 | 2g | 0.392 ± 0.084 | 3g | 0.624 ± 0.023 |
H | Br | 1h | 40.720 ± 2.696 | 2h | 18.450 ± 1.676 | 3h | 5.156 ± 0.011 |
F | F | 1i | 7.721 ± 0.761 | 2i | 0.545 ± 0.029 | 3i | 0.111 ± 0.005 |
Cl | Cl | 1j | 12.910 ± 0.191 | 2j | 0.163 ± 0.025 | 3j | 0.069 ± 0.004 |
Cl | F | 1k | 6.913 ± 0.099 | 2k | 1.691 ± 0.102 | 3k | 1.831 ± 0.126 |
Br | F | 1 l | 1.935 ± 0.083 | 2 l | 3.035 ± 0.091 | 3 l | 1.993 ± 0.005 |