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. Author manuscript; available in PMC: 2018 Jul 13.
Published in final edited form as: J Med Chem. 2018 Jun 25;61(13):5733–5750. doi: 10.1021/acs.jmedchem.8b00777

Table 3.

Antimycobacterial activity (M. bovis BCG), mammalian Vero cell cytotoxicity (IC50) and hemolytic activity (HC50, human RBC) of Series 3 compounds.

graphic file with name nihms976318u4.jpg
No R2 R3 MIC (μM)a Vero IC50
(μM)b 		HC50
(μM)c 		LogPd
MIC50 MIC90
57a graphic file with name nihms976318t83.jpg 4-NO2 10 25 NDe NDe 5.13
57b 5-NO2 7 18 NDe NDe 4.92
57c 6-NO2 0.3 0.8 28 >300 5.87
57d 7-NO2 1.3 3.1 49 >300 6.06
57e 6-CN 0.5 1.2 22 >300 5.53
57f 6-C3H7-n 0.7 1.2 29 27 7.14
57g 6-C3H7-i 0.6 1.6 20 29 6.98
57h 6-BzO 2.2 3.1 27 >300 7.42
12 6-MeO 0.3 0.8 NDe NDe 6.12
58a graphic file with name nihms976318t84.jpg 6-NO2 0.8 1.6 62 >300 5.67
58b 6-CN 2.5 5 59 >300 5.33
58c 6-C3H7-n 3 5 29 31 6.94
58d 6-C3H7-i 3 6 41 56 6.78
58e 6-BzO 4 5.5 36 >300 7.21
1 6-MeO 2 4 NDe NDe 5.92
59a graphic file with name nihms976318t85.jpg 6-NO2 4 5 23 NDe 6.35
59b 6-CN 2 6 22 NDe 6.01
59c 6-C3H7-i 4 6 26 NDe 7.46
52 6-MeO 7 13 NDe NDe 6.60
a–c

As described in footnote of Table 1.

d

Log P values were determined on ACD Labs Physchem History Version 12.5.

e

ND = Not Determined.