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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 18.

SAR and functional activity data of the thiourea analogs.54

graphic file with name nihms-715437-f0139.jpg
Compd R IC50a (μM) Compd R IC50a (μM)
SF-11 4-OC2H5 0.199 158 4-CON(C2H5)2 0.078
150 -H NAc 159 4-SO2N(CH3)2 0.019
151 4-OCH3 1.1 160 4-SO2N(C2H5)2 0.136
152 4-OiPr 1.77 161 3-OCH3 8.162b
153 4-OCF3 1.047 162 3- COOC2H5 0.238b
154 4-nC3H7 0.777 163 3-Cl, 4-N(C2H5)2 0.085
155 4-N(C2H5)2 0.072b 164 3-CN, 4-OC2H5 0.323
156 4-COOC2H5 0.207 165 2-CH3, 4- OC2H5 NA
157 4-CON(CH3)2 0.301 166 2-F, 4- OC2H5 1.35
a

Functional activity using cAMP biosensor assy. All compounds were inactive at the NPY Y1 receptor

b

exhibited partial antagonism

c

not active (NA) at the highest concentration tested (10 μM).