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. Author manuscript; available in PMC: 2018 Apr 15.
Published in final edited form as: Bioorg Med Chem Lett. 2017 Mar 10;27(8):1744–1749. doi: 10.1016/j.bmcl.2017.02.070

Table 3.

a. Primary Carboxamide Replacements

graphic file with name nihms859149u4.jpg
Cmpd X Y SRE.L IC50 (μM) MLM T1/2 (min) ClogP TPSA
1 C=O NH 0.64 1.6 4.25 62.55
16 NH C=O 4.9 3.92 62.6
19 CH2 O 0.81 1.8 4.73 42.7
26b C=O NMe 8.6 4.11 53.8
a

Assay descriptions provided in Table 1.

b

Prepared as in Scheme 1 in ref 9, using N-Me-4-Cl-aniline