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. Author manuscript; available in PMC: 2021 Jul 27.
Published in final edited form as: J Med Chem. 2018 Sep 28;61(19):8875–8894. doi: 10.1021/acs.jmedchem.8b01108

Table 2.

Benzyl Substituents

graphic file with name nihms-1712951-t0010.jpg
Compd R3’ R4’ R5’ EC50 (μM) Act. (%)a
10 Cl F H 2.2 ± 0.52 211 ± 20.5
12 H H H 8.6 ± 1.64 122 ± 17.8
13 H F H 5.9 ± 4.88 130 ± 28.1
14 H Cl H 12.4 ± 2.70 164 ± 15.0
15 H Me H 36.6 ± 17.26 93 ± 13.0
16 H CF3 H 19.6 ± 5.01 148 ± 30.7
17 F F H 5.9 ± 1.33 183 ± 25.3
18 Me F H 4.1 ± 2.00 190 ± 20.6
19 CF3 F H 8.1 ± 0.52 263 ± 52.5
20 graphic file with name nihms-1712951-t0011.jpg F H 11.7 ± 2.74 151 ± 5.0
21 Me F Me 3.7 ± 0.29 270 ± 73.8

Measurements are reported as the mean ± SD of two or more independent experiments, each conducted in duplicate.

a

Activation values represent percentage relative to control.25