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. Author manuscript; available in PMC: 2020 Oct 16.
Published in final edited form as: Bioorg Med Chem. 2010 May 25;18(14):5208–5223. doi: 10.1016/j.bmc.2010.05.057

Table 6.

Effect of the p-substituent of the biphenyl ether residue on activity profiles

graphic file with name nihms-1634538-t0059.jpg
Compds X C3
Configuration
(3R and/or
3S)		 IC50
(nM)
Ca
assay		 Stability in rat
liver
microsomesa
remaining%		 cLog Pb
33 F− (3S) 92 53 7.80
34 Me− (3S) 79 48 8.16
35 MeO− (3S) 130 34 7.58
36 HO− (3S) 42 22 6.99
37 MeHNC(O)− (3S) 33 4 6.38
38 MeSO2HN− (3S) 40 15 6.47
39 H2NO2S− (3S) 28 24 5.82
40 HO2C− (3S) 13 22 5.13
1a H (3RS) 28 33 7.66
a

The data show the remaining% 15 min after incubating with the 0.5 mg/mL rat liver microsomes.

b

Calculated by ADMET predictor (ver. 4.0).