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. Author manuscript; available in PMC: 2022 May 3.
Published in final edited form as: J Med Chem. 2020 Oct 6;63(20):11934–11944. doi: 10.1021/acs.jmedchem.0c01198

Table 1.

MICs in μg/mL (μM) of HSGN-218, analogs, and control antibiotics, against C. difficle ATCC BAA 1801.

graphic file with name nihms-1667791-t0007.jpg
Compound/Control Antibiotic -R1 -R2 -R3 -R4 X MICs in μg/mL (μM)
Compound 12 - - - - - 0.5 (1.4)
1 H H H H CH 2 (5.5)
2 F H H H CH 4 (10.4)
3 Cl H H H CH 4 (10.0)
4 H F H H CH 0.03 (0.08)
5 H Cl H H CH 0.03 (0.08)
6 H OMe H H CH 4 (10.1)
7 H CF3 H H CH 0.015 (0.04)
8 H H F H CH 4 (10.4)
9 H H Cl H CH 2 (5.0)
10 H H CF3 H CH 0.125 (0.29)
11 H H OMe H CH 4 (10.1)
12 H H CH3 H CH 4 (10.5)
13 H H i-Propyl H CH 128 (314.2)
14 Cl H Cl H CH 0.03 (0.07)
15; HSGN-218 H Cl H Cl CH 0.007 (0.02)
16 OMe H H Cl CH 2 (4.7)
17 H H H H N 8 (21.8)
Vancomycin - - - - - 1 (0.7)
Metronidazole - - - - - 0.25 (1.46)
Fidaxomicin - - - - - 0.06 (0.06)