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Table 1 Growth/invasion inhibitory activity of compounds described in this study

From: Macrolides rapidly inhibit red blood cell invasion by the human malaria parasite, Plasmodium falciparum

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
  1. 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