Table 1.
Inhibition of Mtb and Yp Dxr by selected N-acyl and O-linked MEPicides
![]() | ||||
|---|---|---|---|---|
| Cmpd No. | R1 | R2 | Mtb Dxr IC50, µM |
Yp Dxr IC50, µM |
| 1 (Fos) | H | H | 0.44 | 0.71 |
| 2 (FR) | H | CH3 | 2.91 | 0.23 |
| 8b | H | Hexyl | (43)* | (27) |
| 8e | H | Ph | (70) | 4.45 |
| 8f | H | (4-CH3)Ph | (74) | 16.03 |
| 8h | H | CH2CH2CH2Ph | 17.8 | (34) |
| 16d | (4-ipr)Bn | CH3 | 48.4 | 1.19 |
| 16e | CH(CH3)Ph | CH3 | (38.1) | (19) |
| 16g | CH2CH2(4-OH)Ph | CH3 | (59) | (22) |
| 16i | CH2-(1-naphthyl) | CH3 | (29) | 22.35 |
| 16j | CH2-(2-naphthyl) | CH3 | 1.45 | 0.33 |
| 16k | CH2-4-(1,1’-biphenyl) | CH3 | (36.8) | 8.40 |
| 16r | CH2-4-(4’-CF3)-1,1’-biphenyl) | CH3 | (70) | (19) |
Values in parentheses are percent remaining enzyme activity at 100 µM.
