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. Author manuscript; available in PMC: 2018 Oct 1.
Published in final edited form as: Bioorg Med Chem. 2017 Apr 9;25(19):5114–5127. doi: 10.1016/j.bmc.2017.04.005

Table 2.

Enzyme inhibitory and antiviral activity of inhibitors 4a–l.

Entry Inhibitor structure Ki IC50a,b

(nM)
1 graphic file with name nihms870174t9.jpg 30.8 > 1000
2 graphic file with name nihms870174t10.jpg 0.025 69
3 graphic file with name nihms870174t11.jpg 1.61 189
4 graphic file with name nihms870174t12.jpg 0.79 164
5 graphic file with name nihms870174t13.jpg 0.53 221
6 graphic file with name nihms870174t14.jpg 0.76 32
7 graphic file with name nihms870174t15.jpg 0.80 327
8 graphic file with name nihms870174t16.jpg 0.41 33
9 graphic file with name nihms870174t17.jpg 23.6 nt
10 graphic file with name nihms870174t18.jpg 2.50 nt
11 graphic file with name nihms870174t19.jpg 0.49 280
12 graphic file with name nihms870174t20.jpg 0.40 109
a

Darunavir (1) exhibited Ki = 16 pM, antiviral IC50 = 3.2 nM

b

nt = not tested.