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. Author manuscript; available in PMC: 2014 Oct 10.
Published in final edited form as: J Med Chem. 2013 Oct 1;56(19):10.1021/jm401037h. doi: 10.1021/jm401037h

Table 1.

Optimization of distal aryl ring substation for inhibitor 11a

graphic file with name nihms528834t1.jpg
X,X R1 R2 R3 R4 Ki (µM)
11 F,F H H H H 337 ± 60
11a F,F H H H Me 205 ± 1
11b F,F H H H i-Pr 222 ± 1
11c F,F H H Me H 137± 8
11d F,F H H i-Pr H 81 ± 2
11e F,F H OH H H 168 ± 17
11f F,F H OMe H H 271 ± 17
11g F,F H OH i-Pr H 69 ± 9
11h F,F OH H i-Pr H 95 ± 1
11i F,F H OH Et H 124 ± 3
11j F,F H OH t-Bu H 63 ± 1
11k F,F H OH cyclobutyl H 45 ± 2
11l F,F H OH cyclopentyl H 25 ± 4
11m F,F H OH cyclohexyl H 20 ± 3
11n F,F H OH cycloheptyl H 62 ± 1
11o OH,H H OH cyclohexyl H 36 ± 1
a

Ki values were determined using at least 2 independent measurements.