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. Author manuscript; available in PMC: 2017 Jun 1.
Published in final edited form as: Bioorg Med Chem. 2016 Apr 2;24(11):2451–2465. doi: 10.1016/j.bmc.2016.04.006

Table 5.

Stability of select compounds to mouse and human liver microsomes

T. b. rhodesiense a
MLM
 HLM
Compd
 IC50 (μM)
 Microsomal t1/2 (min)b
 Substrate remainingc
 Microsomal t1/2 (min)b
 Substrate remainingc
1 0.632 1.1 43% 28 80%
9 0.156 1.9 29% 34 96%
10 0.233 3.2 48% 22 75%
16 0.162 5.5 22% 50 67%
30 0.460 1.5 60% 36 93%
43 0.164 0.6 0.4% 8.0 104%
44 0.125 0.5 89% 13 88%
46 0.0204 1.7 102% 9.1 104%
57 0.104 7.6 97% 34 98%
60 0.129 11 106% 27 107%
62 0.325 4.7 62% 24 69%
65 0.149 1.6 83% 9.4 24%
67 0.0495 0.3 101% 11 100%
68 0.0517 1.8 105% 17 103%
70 0.0090 1.6 90% 4.9 102%
a

Trypanosoma brucei rhodesiense (STIB900), data reproduced from Table 1

b

Microsomal t1/2 was determined in the presence of the NADPH cofactor.

c

Substrate concentrations were determined in incubations without NADPH after 60 min and normalized to concentrations at time zero.