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. Author manuscript; available in PMC: 2023 Oct 27.
Published in final edited form as: J Med Chem. 2022 Oct 11;65(20):13910–13934. doi: 10.1021/acs.jmedchem.2c01151

Table 3.

Additional Aryl 4-Aminoquinoline Analogues

graphic file with name nihms-1861478-t0004.jpg
compound R1 R2 R3 MIC (μg/mL) clog P
21 CF3 H 3,4-difluorophenyl 0.125–0.25 6.6
22 CF3 H 3,4-dichloropheyl 0.0625 7.7
31 CF3 H 5-(trifluoromethyl)pyridin-2-yl 0.25 6.1
32 OCF3 H 3,4-dichlorophenyl 0.5–1 8.2
33 OCF3 H 3-(trifluoromethoxy)phenyl 1 7.9
34 OCF3 H 5-(trifluoromethyl)pyridin-2-yl 1 6.5
35 OMe H 3,4-dichlorophenyl 2 6.0
36 OMe H 3,4-difluorophenyl >32 4.9
37 OMe H 3-(trifluoromethoxy)phenyl >32 5.7
38 OMe H 5-(trifluoromethyl)pyridin-2-yl 32 4.3
39 S(O)2N(Me)2 H 3,4-difluorophenyl >32 5.1
40 S(O)2N(Me)2 H 3-(trifluoromethoxy)phenyl 8 5.9
41 S(O)2N(Me)2 H 5-(trifluoromethyl)pyridin-2-yl 8 4.5
42 H OCF3 3,4-dichlorophenyl 0.5 8.2
43 H OCF3 3-(trifluoromethoxy)phenyl 1 7.8
44 H OCF3 5-(trifluoromethyl)pyridin-2-yl 1 6.5
45 H CF3 3,4-dichlorophenyl 0.5–2 8.2
46 H CF3 3-(trifluoromethoxy)phenyl 1 7.9
47 H CF3 5-(trifluoromethyl)pyridin-2-yl 0.5 6.5