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Table 1 Activity data for anti-malarial drugs

From: Identification of inhibitors of Plasmodium falciparum gametocyte development

COMPOUND 3D7a NF54-pfs16-GFPa NF54-pfs16-GFPb (I-III)/ABS (IV-V)/ABS
ABS early (I-III) gam late (IV-V) gam
4-Aminoquinolines
Amodiaquine 255 (65) 242 (110) 87% 0.9  
Naphthoquines 411 (82) 483 (330) NA 1.2  
AQ-13 183 (0.01) 453 (230) 82% 2.5  
Piperaquines 1880 (210) 3990 (2800) 43% 1.6  
Hydroxychloroquines 966 (130) 1340 (140) 45% 1.4  
Pyronaridine 299 (69) 250 (96) 4260 (240) 0.8 14.2
8-Aminoquinolines
Pamaquine 88% 79% NA   
Primaquine 7120 (1500) NA 74%   
Tafenoquine 5650 (1600) 4800 (1500) 4620 (1600) 0.8 0.8
NPC-1161B 3360 (860) 2180* 4850 (2700) 0.6 1.4
Endoperoxides
Artemether 25.8 (11) 11 (2.8) 3.13 (0.7) 0.4 0.1
Artenimol (DHA) 2.08 (0.6) 18.3 (17) 2.17 (1.2) 8.8 1.0
Artesunate 6.7 (1.6) 3.8 (0.28) 2.53 (1.10) 0.6 0.4
Artemisinin 41.6 (12) 12.1 (14) 5.47 (2.0) 0.3 0.1
Artemisone 3.72 (0.14) 2.4 (0.85) 1.7 (0.46) 0.6 0.5
Anti folates
Pyrimethamine 21.5 (0.07) NA NA   
Chlorproguanil 6250 (520) 108% 4340 (840)   0.7
Proguanil HCl 78% 6540* 84%   
Dapsone NA NA NA   
Sulphonamides
Sulfadiazine NA NA NA   
Sulfamethoxazole NA NA NA   
Sulfadoxine NA NA NA   
Amino alcohols
Halofantrine 136 (66) 135 (98) 31.9 (11) 1.0 0.2
Lumefantrines 137 (70) 107 (137) 2.07 (0.55) 0.8 0.0
Mefloquine (Racemic) 158 (33) 223 (120) 100 (3.6) 1.4 0.6
Mefloquine (+ RS) 133 (41) 226 (76) 134 (110) 1.7 1.0
Quinine sulfate 217 (0.7) 2110 (280) 318 (180) 9.7 1.5
Antibiotics
Trimethoprim 3740 (120) NA NA   
Thiostrepton 913 (210) 959 (570) 556 (58) 1.1 0.6
Clindamycin 325 (64) NA NA   
Cis-mirincamycin (HCl) NA NA 64%   
Trans-mirincamycin (HCl) 86% NA 66%   
Tetracycline 2270 (170) NA NA   
Other
Fosmidomycin mono sodiums 91% NA NA   
Methylene blue trihydrate 21.9 (0.07) 280 (130) 287 (100) 12.8 13.1
Pentamidine 697 (36) 1560 (620) 2850 (540) 2.2 4.1
  1. ABS Asexual blood stage, gam gametocyte, an = 2, bn = 3. IC50 nM (SD), * n = 1 only, NA Not active at 40 μM, % at 40 μM. sPotential solubility issues with stock compounds in DMSO.