Table 2.
Structure-activity analysis of non-symmetrical DMTU analogs.
| Inhibitor | Structure | R | UT-A1 IC50 (mM) | UT-B IC50 (mM) |
|---|---|---|---|---|
| 9 |
|
aniline | 8.8 ± 0.3 | 14 ± 1 |
| 10 | 2-amino-benzimidazole | 2.2 ± 0.3 | 4.7 ± 1.4 | |
| 11 | 4-amino-pyridine | 5.3 ± 0.6 | 1.6 ± 0.3 | |
| 12 | 4-amino-cyclohexyl | 3.7 ± 0.2 | 5.2 ± 0.6 | |
| 13 | 4-fluoro-aniline | 13 ± 3 | >15 | |
| 14 | 4-chloro-aniline | 6.3 ± 1.3 | >15 | |
| 15 | 4-bromo-aniline | 3.8 ± 0.6 | 2.4 ± 0.2 | |
| 16 | 4-trifluoromethyl-aniline | 15 ± 0.3 | >15 | |
| 17 | 4-carboxy-aniline | 7.5 ± 1.0 | 3.6 ± 0.6 | |
| 18 | 4-nitro-aniline | 1.3 ± 0.3 | 10 ± 1 | |
| 19 | 4-methoxy-aniline | >15 | >15 | |
| 20 | 4-dimethylamino-aniline | >15 | >15 | |
| 21 | 3,4-dichloro-aniline | 1.5 ± 0.4 | 0.4 ± 0.1 | |
| 22 | 2,3-dichloro-aniline | >15 | >15 | |
| 23 | 2,6-dichloro-aniline | >15 | >15 | |
| 24 | 2,4,6-trichloro-anilne | 5.9 ± 1.1 | >15 | |
| 25 | 4-chloro-benzylamine | >15 | >15 | |
| 26 | 4-pyridine | >15 | 2.8 ± 0.5 | |
| 27 | 3-pyridine | >25 | 10 ± 2 |