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. Author manuscript; available in PMC: 2016 Jun 15.
Published in final edited form as: Bioorg Med Chem Lett. 2015 Apr 11;25(12):2594–2598. doi: 10.1016/j.bmcl.2015.03.074

Table 4.

SAR of central amide N-substituent

graphic file with name nihms689082u5.jpg
Cmp R4 IC50 (μM)a
1a
Ar2=A
graphic file with name nihms689082t26.jpg 0.055±0.014
4b
Ar2=A
graphic file with name nihms689082t27.jpg 7.5
4d
Ar2=A
graphic file with name nihms689082t28.jpg 1.6
4f
Ar2=B
graphic file with name nihms689082t29.jpg 0.84
4a
Ar2=A
graphic file with name nihms689082t30.jpg 19
4c
Ar2=A
graphic file with name nihms689082t31.jpg 0.11
4e
Ar2=A
graphic file with name nihms689082t32.jpg >25
a

Average of at least two measurements in DiI uptake assay, ± standard error of mean when n > 2.