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. Author manuscript; available in PMC: 2015 Dec 8.
Published in final edited form as: Bioorg Med Chem Lett. 2013 Dec 4;24(2):430–441. doi: 10.1016/j.bmcl.2013.11.061

Table 15.

SAR data of 4-aminopiperidine analogs.53

graphic file with name nihms-715437-f0126.jpg
Compd R Ar fpKia cLogP Solubility(μg/mL)
137 Et Ph 5.7 3.96 nt
138 iPr Ph 6.0 4.26 nt
139 n-Pr Ph 6.6 4.48 nt
140 i-Bu Ph 7.1 4.88 nt
141 graphic file with name nihms-715437-t0127.jpg Ph 6.9 4.4 121
142 graphic file with name nihms-715437-t0128.jpg (m-Me)Ph 7.6 4.9 268
143 graphic file with name nihms-715437-t0129.jpg (m-CF3)Ph 7.7 5.28 219
144 graphic file with name nihms-715437-t0130.jpg graphic file with name nihms-715437-t0131.jpg 5.9 2.9 nt
145 graphic file with name nihms-715437-t0132.jpg graphic file with name nihms-715437-t0133.jpg 6.4 2.9 112
146 graphic file with name nihms-715437-t0134.jpg graphic file with name nihms-715437-t0135.jpg 6.1 2.44 248
a

Functional activity against human Y2 receptors using [35S]GTPγS binding assay.