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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.