Structures of MDL860 analogs, anti-TB (H37Rv strain) activity and cytotoxicity (Vero cell).
| Cpd No. | Structure | MIC (μM) | IC50 (μM) | |
|---|---|---|---|---|
| GASc | 7H12d | Vero cell | ||
| 13 | MDL860 | 45 | >50 | >50 |
| 26 a |
|
2 | 2.4 | >100 |
| 27 a |
|
5 | >5 | >100 |
| 28 a |
|
>5 | >5 | >100 |
| 29 b |
|
5 | >5 | 29 |
| 30 b |
|
>5 | >5 | >100 |
| 31 b |
|
>5 | >5 | >100 |
| 32 a |
|
>5 | >5 | >100 |
| 33 a |
|
5 | >5 | >100 |
| 34 b |
|
2 | >5 | >100 |
| 35 b |
|
3 | >5 | >100 |
| 36 b |
|
>5 | >5 | >100 |
| 4 | PA-824 | 0.2 | 0.08 | >100 |
a
Reaction condition: N-methylmorpholine, DIPEA, 80 °C.
b
Reaction condition: NaOH, DMF, 100 °C.
c
GAS: glycerol–alanine salts medium.
d
7H12: 7H9 medium + casitone, palmitic acid, albumin, and catalase.