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. Author manuscript; available in PMC: 2021 May 21.
Published in final edited form as: Cell Chem Biol. 2020 Mar 19;27(5):560–570.e10. doi: 10.1016/j.chembiol.2020.02.007

Table 2.

Key Properties of Select Transposed Indazoles

graphic file with name nihms-1572786-t0008.jpg
Compound R1 R2 MIC H37Rv (μM) Vero CC50(μM) MLM t1/2(min) Kinetic Aqueous Solubility (μM) AUC0–5h (h×ng/mL) t > MIC (h) Clung/Cplasma at 5 h
5ga Me Me 0.20 94 11.5 76.8 23,003 5 1.0
12 (JSF-3285) Me CH2F 0.20 170 28.4 175 59,323 5 0.75
13 Me Et 0.12 89 3.26 476 13,943 5 1.3
14 Cl Me 0.39 22 32.1 443 51,745 5 0.60
15 Me CF3 0.25 >160 nd nd 28,361 5 0.95
16 Cl CF3 0.20 >150 nd nd 21,989 5 1.2
17 Cl Et 0.39 170 nd nd 34,840 5 1.7
18 Cl CH2F 0.20 160 nd nd nd nd nd
19 CF3 Me 25 78 nd nd nd nd nd
20 CF3 Et 12 37 nd nd nd nd nd

nd, not determined.