Table 2. Aminoguanidine Methyl, Methoxy, Fluoromethyl, Fluoromethoxy, and Nitrile Seriesa.
| compound | R1 | R2 | IC50 D6 (nM) | IC50 Dd2 (nM) | IC50 Tm90–C2B (nM) | IC50 A6 (nM) | IC50 cytotoxicity (μM) | IVTI |
|---|---|---|---|---|---|---|---|---|
| 10 | 4-CH3 | H | 905 | 2427 | 2529 | >5000 | 43 | 48 |
| 11 | 4-OCH3 | H | 263 | 1602 | >5000 | 289 | >200 | >100 |
| 12 | 4-CF3 | H | 614 | 1536 | 2742 | 567 | 40 | 65 |
| 13 | 4-CF3 | CH3 | 211 | 414 | 451 | 283 | 114 | >100 |
| 14 | 2-OCF3 | H | 1080 | 2328 | >5000 | 391 | 156 | >100 |
| 15 | 3-OCF3 | H | 670 | 1571 | 2988 | 689 | 61 | 91 |
| 16 | 4-OCF3 | H | 39 | 83 | 114 | 52 | 11 | >100 |
| 17 | 4-OCF3 | CH3 | 140 | 526 | 458 | 182 | 9 | 64 |
| 18 | 4-OCHF2 | H | 71 | 191 | 193 | 87 | 19 | >100 |
| 19 | 4-OCHF2 | CH3 | 99 | 403 | 315 | 171 | 3 | 30 |
| 20 | 2-CN | H | 1024 | 2097 | 1990 | 969 | 31 | 30 |
| 21 | 3-CN | H | 7 | 20 | 31 | 24 | 7 | >100 |
| 22 | 4-CN | H | 58 | 166 | 312 | 76 | >200 | >100 |
| 23 | 3-CN | CH3 | 47 | 70 | 104 | 17 | 9 | >100 |
| 1 | 3-CN, 4-F | H | 4 | 12 | 16 | 14 | 8 | >100 |