Table 4. Additional Activity Data for Selected Analogs from Each Series.
| antiparasitic
IC50 (μM) (pIC50 ± SE) |
antibacterial MIC (μg/mL) | |||
|---|---|---|---|---|
| compound | G. lambliaa | E. histolyticab | ESKAPEc | antifungald MIC (μg/mL) |
| pretomanid 2 | 3.0 (5.5 ± 0.02) | 9.3 (5.0 ± 0.03) | >32 | >32 |
| 16a | 5.0 (5.3 ± 0.05) | >50 (<4.3) | >32 | >32 |
| 16b | 3.5 (5.5 ± 0.01) | >50 (<4.3) | >32 | >32 |
| 16d | 1.7 (5.8 ± 0.03) | >50 (<4.3) | >32 | >32 |
| Series 1 | ||||
| 17a | 18 (4.7 ± 0.03) | >50 (<4.3) | >32 | >32 |
| 17d | >50 (<4.3) | >50 (<4.3) | >32 | >32 |
| 17e | >50 (<4.3) | >50 (<4.3) | >32 | >32 |
| 17i | >50 (<4.3) | >50 (<4.3) | >32 | >32 |
| 17k | 23 (4.6 ± 0.02) | >50 (<4.3) | >32 | >32 |
| Series 2 | ||||
| 26a | 40 (4.4 ± 0.04) | >50 (<4.3) | >32 | >32 |
| 26b | 19 (4.7 ± 0.04) | >50 (<4.3) | >32 | >32 |
| 26j | 7.1 (5.1 ± 0.02 | >50 (<4.3) | >32 | >32 |
| 26k | 2.4 (5.6 ± 0.04) | >50 (<4.3) | >32 | >32 |
| Series 3 | ||||
| 34a | 0.5 (6.3 ± 0.11) | >50 (<4.3) | >32 | >32 |
| 3d | 37 (4.4 ± 0.08) | >50 (<4.3) | >32 | >32 |
| 34k | 1.8 (5.7 ± 0.09) | >50 (<4.3) | >32 | >32 |
| 34p | 5 (5.3 ± 0.03) | >50 (<4.3) | >32 | >32 |
a
WB.
b
HM1:IMSS.
c
ESKAPE pathogens include Staphylococcus aureus (MRSA ATCC 43300), Escherichia coli (ATCC 25922), Klebsiella pneumoniae (ATCC 700603), Acinetobacter baumannii (ATCC 19606), and Pseudomonas aeruginosa (ATCC 27853).
d
Candida albicans (ATCC 90028) and Cryptococcus neoformans var. grubii H99 (ATCC 208821).