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. Author manuscript; available in PMC: 2019 Nov 8.
Published in final edited form as: J Med Chem. 2018 Oct 19;61(21):9647–9665. doi: 10.1021/acs.jmedchem.8b01126

Table 3.

ADME and Pharmacokinetic properties of 5,7-substituted 8-hydroxyquinolines

Example Hepatocyte Stability (Rat) (μL/min/106 cells) Rat PKb
%F T1/2 (h) Clp (ml/min/kg) Vss (L/kg)
11 24 0.18 26 1.8
12 177
15 39
16 228
17 46
18 12 66 3.5 13 3.8
19 4 23 8.9 0.31 0.23
20 15 100 4.5 12 3.5
21 36 34 0.26 27 1.2
22 78 45 0.31 25 0.67
25 19 32 7.7 0.62 0.41
26 18 37 11 0.3 0.3
28 21 73 2.8 11 2.2
29 14 33 8.6 1 0.8
30 103
b

Rat pharmacokinetics after a 1mpk iv dose (n=3) and 3 or 10 mpk oral dose (n=3)