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. 2021 Mar 16;7(7):1956–1968. doi: 10.1021/acsinfecdis.1c00001

Table 2. Aminoguanidine Methyl, Methoxy, Fluoromethyl, Fluoromethoxy, and Nitrile Seriesa.

compound R1 R2 IC50 D6 (nM) IC50 Dd2 (nM) IC50 Tm90–C2B (nM) IC50 A6 (nM) IC50 cytotoxicity (μM) IVTI
10 4-CH3 H 905 2427 2529 >5000 43 48
11 4-OCH3 H 263 1602 >5000 289 >200 >100
12 4-CF3 H 614 1536 2742 567 40 65
13 4-CF3 CH3 211 414 451 283 114 >100
14 2-OCF3 H 1080 2328 >5000 391 156 >100
15 3-OCF3 H 670 1571 2988 689 61 91
16 4-OCF3 H 39 83 114 52 11 >100
17 4-OCF3 CH3 140 526 458 182 9 64
18 4-OCHF2 H 71 191 193 87 19 >100
19 4-OCHF2 CH3 99 403 315 171 3 30
20 2-CN H 1024 2097 1990 969 31 30
21 3-CN H 7 20 31 24 7 >100
22 4-CN H 58 166 312 76 >200 >100
23 3-CN CH3 47 70 104 17 9 >100
1 3-CN, 4-F H 4 12 16 14 8 >100
a

See Table 1 legend and Methods.