Skip to main content
. 2011 Aug 10;6(10):1832–1840. doi: 10.1002/cmdc.201100278

Table 5.

Core ring variation in compounds 42–48

Inline graphic
Compd Ring A R EC50 [μm] CLi [mL min−1 g−1][b]
T. b. brucei[a] MRC-5 Human Mouse
3 Inline graphic methyl 0.052 40 3.3 3.6
42 Inline graphic methyl 16.6 50 ND ND
43 Inline graphic methyl 50 50 ND ND
44 Inline graphic H 17.7 50 ND ND
45 Inline graphic H 16.3 50 0.6 ND
46 Inline graphic methyl 0.88 9.8 2.2 6.8
47 Inline graphic methyl 5.4 8.3 1.4 7.4
48 Inline graphic – 9.9 50 ND ND
[a]

Hill slopes in the range of 1.1–8.8.

[b]

Microsomal intrinsic clearance; ND: not determined.