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. Author manuscript; available in PMC: 2022 Jun 24.
Published in final edited form as: J Med Chem. 2021 Jun 3;64(12):8287–8302. doi: 10.1021/acs.jmedchem.1c00279

Table 2.

α-Cyano alcohol derived γ-hydroxyamines.

graphic file with name nihms-1732961-t0003.jpg
Compound R3 R1 R2 IC50 (nM) Compound R3 R1 R2 IC50 (nM)
Racemic emixustat graphic file with name nihms-1732961-t0004.jpg H H 172 ± 29 (R)-MB-001 graphic file with name nihms-1732961-t0005.jpg H H 323 ± 145
49 4-F H 95 ± 5 53 4-F H 284 ± 20
50 5-F H 201 ± 23 54 5-F H 292 ± 89
51 6-F H 145 ± 9 55 6-F H 124 ± 21
52 2-F H 358 ± 42 56 2-F H 169 ± 13
58 H D 190 ± 15 57 graphic file with name nihms-1732961-t0006.jpg H H 103 ± 29
59 H D 269 ± 40