Entry | Compound | R | IC50 (µΜ) | Yield (%)c | |
---|---|---|---|---|---|
1 | 10a | H | 35.6 ± 8.9 | 65 | |
2 | 10b | 3-Me | 58.9 ± 7.5 | 71 | |
3 | 10c | 4-Me | > 250 | 70 | |
4 | 10d | 4-iPr | 86.5 ± 7.3 | 68 | |
5 | 10e | 3-OMe | 35.7 ± 3.9 | 72 | |
6 | 10f | 4-OMe | 25.2 ± 2.5 | 66 | |
7 | 10 g | 4-F | 37.5 ± 7.2 | 79 | |
8 | 10 h | 2-Cl | 14.9 ± 1.9 | 62 | |
9 | 10i | 3-Cl | > 250 | 60 | |
10 | 10j | 4-Cl | 21.0 ± 5.3 | 74 | |
11 | 10k | 4-Br | 1.7 ± 0.12 | 61 | |
12 | 10 L | 3,5-diCl | 14.1 ± 3.3 | 64 | |
13 | 10 m | 3,4-diCl | 27.7 ± 3.0 | 78 | |
14 | 10n | 3-CN | > 250 | 70 | |
15 | 10o | 4-CN | 28.9 ± 3.3 | 77 | |
16 | 10p | 3-NO2 | 84.0 ± 13.2 | 81 | |
17 | 10q | 4-NO2 | 47.1 ± 5.6 | 73 | |
18 | 10r | 3-Me-4-NO2 | > 250 | 65 | |
19 | Acarbose | 170.5 ± 23.1 |