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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 6.

Heteroatom Exchanges

graphic file with name nihms-1861478-t0007.jpg
Compound X Y Z R MIC μg/mL cLogP
80 CH O CH 3-chlorophenyl >32 6.8
81 CH O CH 3-fluorophenyl >32 6.2
82 CH O CH 3,4-dichlorophenyl >32 7.4
83 CH O CH 3-(trifluoromethoxy)phenyl >32 7.1
84 CH NMe CH 4-trifluoromethylphenyl >32 7.4
85 CH N(C=O) CH 5-(trifluoromethyl)pyridin-2-yl >32 5.3
89 N NH CH 3,4-dichlorophenyl 0.5 6.9
90 N NH CH 3-(trifluoromethoxy)phenyl 1 6.6
91 N NH CH 5-(trifluoromethyl)pyridin-2-yl 2 5.1
94 N NH N 3,4-difluorophenyl 32 4.0
95 N NH N 5-(trifluoromethyl)pyridin-2-yl >32 5.8
graphic file with name nihms-1861478-t0008.jpg
Compound R MIC μg/mL cLogP
100 3,4-difluorophenyl >32 4.8
101 5-(trifluoromethyl)pyridin-2-yl >32 4.1