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. Author manuscript; available in PMC: 2020 Jul 12.
Published in final edited form as: J Med Chem. 2020 May 26;63(11):6179–6202. doi: 10.1021/acs.jmedchem.0c00539

Table 5.

In Vivo Blood-Stage Antimalarial Efficacy against P. yoelii in Mice

compd blood-stage efficacy vs. P. yoelii (4 days)
ED50 (mg/kg/d) ED90 (mg/kg/d)
T31 1.0 1.6
18a 0.52 0.82
19 1.8 1.9
21 4.5 6.8
20b 1.8 3.6
22c,d 0.18 0.32
23 5.0 9.8
24 0.55 0.86
25 3.7 6.3
26c 0.045 0.098
27b 2.1 7.2
28 >30 >30
29b,c 0.28 0.32
30 3.6 12
31 >30 >30
32 23 >30
33 5.4 8.9
34 2.8 7.5
35 >30 >30
36 >30 >30
37 1.8 14
38 0.75 3.9
39 1.3 7.3
40 0.16 3.6
41 >30 >30
42 >30 >30
43 0.23 9.8
44 0.23 0.79
45 0.96 2.2
46 >30 >30
47 1.1 2.3
48 4.1 7.4
49 3.7 6.7
50 6.8 >30
51 6.1 >30
52 >30 >30
53 10 19
54 27 >30
55 15 28
56 17 32
57 9.2 14.7
58 8.9 16
68 1.6 1.8
69 0.30 1.0
70 >30 >30
73 4.6 6.6
74 3.9 5.8
77 5.4 6.9
86 7.2 18
87 0.34 0.42
88c 0.36 0.45
89 0.28 7.7
90 0.17 0.63
91 0.15 0.56
92 0.38 0.47
93 8.0 15
99 6.1 12
100 2.8 13
101 >10 >10
102 >10 >10
107 0.15 1.5
108 <5.0 <5.0
109 9.5 16
CQ 1.5 3.3
a

curative at 5 mg/kg/d;

b

curative at 30 mg/kg/d;

c

curative at 10 mg/kg/d;

d

curative at 3.0 mg/kg/d.