Table 1.
Synthesis and inhibition by lead analogs.
 | |||||
| Compound | R1 | R2 | E. coli IC50/μM1 | Synthesis2 | Yield% |
| 1 |  |
 |
32 ± 6 | A/B | 25/25 |
| 2 |  |
 |
>100 | n/a | commercial |
| 3 |  |
 |
44 ± 4 | A | 27 |
| 4 |  |
 |
22 ± 3 | B | 34 |
| 5 |  |
 |
17 ± 2 | n/a | commercial |
| 6 |  |
 |
>100 | n/a | commercial |
| 7 |  |
 |
18 ± 1 | C | 21 |
| 8 |  |
 |
15 ± 2 | B | 31 |
| 9 |  |
 |
>100 | n/a | commercial |
| 10 |  |
 |
33 ± 4 | A | 32 |
| 11 |  |
 |
15 ± 2 | n/a | commercial |
| 12 |  |
 |
19 ± 3 | B | 12 |
| 13 |  |
 |
40 ± 3 | B | 33 |
| 14 |  |
 |
9 ± 1 | B | 39 |
1IC50 values are the avearge of 4 determinations and the errors are ± 1 SD. 2A-NaOEt conditions. B-CS2CO3 conditions, C-NaOMe conditions.