Table 1.
Growth/invasion inhibitory activity of compounds described in this study
| Compound number | Compound abbreviation | Compound name | Lactone ring size | IIA IC50 (μM) | 40 hour IC50 (μM) | 90 hour IC50 (μM) | 120 hour IC50 (μM) |
|---|---|---|---|---|---|---|---|
| 1 | AZRa | Azithromycin | 15 | 10 | 6 | 7 | 0.04 |
| 2 | AZR-desclada | - | 15 | 50 | 39 | 31 | ND |
| 3 | AZR-desglycana | - | 15 | >1,600 | >500 | 285 | ND |
| 1 | AZRb | Azithromycin | 15 | 38 | 12 | 7 | 0.1 |
| 4 | 12eb,c | - | 15 | 15 | 1 | 0.6 | 0.16 |
| 5 | 1jb,c | - | 15 | 7 | 0.9 | 0.7 | 0.16 |
| 6 | 11cb,d | - | 15 | 28 | ND | 0.9 | ND |
| 7 | 7/47b,e | - | 15 | 52 | ND | 5 | ND |
| 8 | 7/25b,e | - | 15 | 73 | ND | 10 | ND |
| 9 | ERYa | Erythromycin | 14 | 420 | 230 | 52 | ND |
| 10 | ERY-desclada | - | 14 | ND | 288 | 185 | ND |
| 11 | ERY-oximea | - | 14 | 150 | 85 | 24 | ND |
| 12 | ROXa | Roxithromycin | 14 | 83 | 70 | 27 | ND |
| 13 | DIRa | Dirithromycin | 14 | 521 | 15 | 8 | ND |
| 14 | Meg-ERYa,f | 6-0-megosaminyl-erythromycin | 14 | 13 | ND | ND | ND |
| 15 | SPIa | Spiramycin | 16 | 123 | 15 | 13 | ND |
| 16 | CLIa | Clindamycin | NA | 743 | ND | ND | ND |
| D10-AZRr (delayed death, resistant) comparison | |||||||
| 1 | AZRa | Azithromycin | 15 | - | - | - | 0.16g,h |
| 1g | AZRa | Azithromycin | 15 | 25 | ND | ND | 9h |
aVehicle was ethanol; bvehicle was dimethyl sulfoxide (DMSO); cfrom Bukvic et al. [44]; dfrom Peric et al. [42]; efrom Hutinec et al. [43]; ffrom Goodman et al. [41]. All IC50s are for the D10-PfPHG line used throughout this study, with the exception of gwhich were undertaken with the D10 azithromycin-resistant line (D10-AZRr) made as per Goodman et al. [41]. All assays were measured by flow cytometry, with the exception of hwhich were measured by hypoxanthine uptake assays. Desclad, descladinosyl; desglycan, descladinosyl and desosaminyl; NA, not applicable; ND, not done