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Table 1 In vitro efficacy of antimalarials and azithromycin analogues against Plasmodium spp. parasites

From: Retargeting azithromycin analogues to have dual-modality antimalarial activity

cmpnd R3 class R4 class R5 class In-cycle (44 hr) growth D10-PfPHG IC50 (μMa, ±SEM) In-cycle (44 hr) growth DD2 IC50 (μMb, ±SEM) Invasion inhibition D10-PfPHG IC50 (μMc, ±SEM) In-cycle (24 hr) growth PkYH1 IC50 (μMd, ±SEM)
AZR Me Me H 11.31 (0.49) 15.6 (2.1) 10 (1.4) 16 (1.8)
CQ   0.052 (0.006) 0.31 (0.31) ND 0.017 (0.005)
QN 0.39 (0.07) ND ND ND
DHA 0.0008 (0.0001) ND ND 0.0024 (0.001)
1 Chloroquinoline Me H 0.019 (0.004) 0.082 (0.02) ND 0.2 (0.005)
56 Me Chloroquinoline H 0.011 (0.002) 0.093 (0.02) 3.2 (0.39) 0.031 (0.008)
59 Me Chloroquinoline H 0.073 (0.02) 0.049 (0.005) ND ND
66 Me Me Chloroquinoline 0.007 (0.001) 0.043 (0.002) ND 0.012 (0.002)
69 Me Me Chloroquinoline 0.031 (0.004) ND ND ND
70 Me Me Chloroquinoline 0.05 (0.006) ND ND ND
72 Me Me Chloroquinoline 0.27 (0.01) 0.065 (0.004) 1.7 (0.02) 0.15 (0.06)
8 Quinoline Me H 0.41 (0.02) 0.52 (0.1) 4.4 (1.2) 0.15 (0.01)
10 Quinoline Me H 0.48 (0.04) 0.748 (0.1) ND 0.1 (0.005)
58 Me Quinoline H 0.048 (0.004) 0.056 (0.01) ND 0.071 (0.013)
71 Me Me Quinoline 0.053 (0.005) 0.16 (0.02) ND 0.041 (0.005)
73 Me Me Quinoline 0.31 (0.02) 0.48 (0.2) ND 0.248 (0.07)
3 Naphthalene Me H 0.183 (0.02) 0.32 (0.07) 1.8 (0.5) 0.095 (0.02)
4 Naphthalene Me H 0.19 (0.01) ND 2.0 (0.2) ND
15 Naphthalene Me H 0.67 (0.07) 0.4 (0.1) 3.6 (0.4) 0.32 (0.12)
5 Substituted phenyl thiourea Me H 0.2 (0.01) 0.4 (0.05) 1.61 (0.02) 0.082 (0.02)
6 Substituted phenyl thiourea Me H 0.28 (0.05) 0.27 (0.07) ND 0.16 (0.03)
9 Substituted phenyl thiourea Me H 0.44 (0.07) 0.24 (0.04) ND 0.016 (0.005)
17 Substituted phenyl thiourea Me H 0.7 (0.05) 0.54 (0.06) ND 0.36 (0.01)
  1. a Drug treatment of intracellular growth, from rings to late schizonts, with no rupture cycle for D10-PfPHG (P. falciparum, 0–44 hrs). Data represents the mean of 3 or more experiments
  2. b Drug treatment of intracellular growth, from rings to late schizonts, with no rupture cycle for DD2 (P. falciparum, 0–44 hrs). Data represents the mean of 3 or more experiments
  3. c Drug treatment of D10-PfPHG merozoites prior to addition of RBCs. Parasitemia was measured by flow cytometry ~ 30 min post invasion. Data represents the mean of 2 (for compounds 4 and 5) or 3 experiments
  4. d Drug treatment of intracellular growth, from rings to late schizonts, with no rupture cycle for P. knowlesi YH1 (P. knowlesi, 0–24 h). Data represents the mean of 2 or more experiments