Skip to main content
. 2019 Dec 26;6(2):173–179. doi: 10.1021/acsinfecdis.9b00396

Table 1. Initial Benzoxaborole–Benzimidazole Amide Leadsa.

graphic file with name id9b00396_0004.jpg

ID link atom n R O. volvulus IC50 (μM)31,32 G2/M arrest IC50 (μM)33 MDCK-MDR1 Papp (A-B, ×106 cm/s)3436
1 NA NA NA 0.004 0.67 15.6
7a 6 0   4.55 >100 NT
7b 6 0 3,3-Me2 >10 NT NT
8a 6 1 3,3-Me2 0.300 13 0.8
8b 3 1   0.426 10 NT
8c 6 1   0.421 >100 NT
8d 5 1 3,3-Me2 0.042 2.54 0.5
9a 6 2 3,3-Me2 0.004 0.555 0.7
12a 6 0 3,3-Me2 >10 >100 NT
a

NT = not tested.