Table 1.
Compd | Type | R2 | R3 | R4 | R5 | R | pIC50 ± SE | IC50 (μM) |
---|---|---|---|---|---|---|---|---|
Peptide | 5.92 ± 0.04 | 1.2 | ||||||
⁎1a | I | Me | H | H | Me | 4.42 ± 0.08 | 37 | |
⁎1b | 4.28 ± 0.06 | 53 | ||||||
⁎1c | 3.96 ± 0.14 | 108 | ||||||
⁎1d | 3.98 ± 0.10 | 103 | ||||||
27 | II | — | — | — | — | H | 3.75 ± 0.15 | 178 |
28 | II | — | — | — | — | Thiazol-2-yl | 3.89 ± 0.06 | 129 |
29 | II | — | — | — | — | 4-Me-thiazol-2-yl | 4.53 ± 0.06 | 30 |
30 | II | — | — | — | — | 5-Me-isoxazol-3-yl | 4.37 ± 0.07 | 43 |
31 | I | H | H | H | H | — | 4.63 ± 0.04 | 23 |
32 | I | H | Me | H | H | — | 4.89 ± 0.04 | 13 |
33 | I | H | H | Me | H | — | 4.96 ± 0.04 | 11 |
34 | I | Me | H | Me | H | — | 4.83 ± 0.04 | 15 |
35 | I | H | Me | Me | H | — | 5.02 ± 0.04 | 10 |
36 | I | H | H | iPr | H | — | 5.35 ± 0.04 | 4 |
37 | I | H | H | CF3 | H | — | 4.55 ± 0.07 | 28 |
38 | I | H | CF3 | H | CF3 | — | 5.05 ± 0.03 | 9 |
39 | I | H | H | Cl | H | — | 4.76 ± 0.03 | 17 |
40 | I | H | H | Br | H | — | 5.14 ± 0.03 | 7 |
Compounds 1a–d were purchased from Asinex.