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. Author manuscript; available in PMC: 2014 Nov 1.
Published in final edited form as: Bioorg Med Chem Lett. 2013 Sep 10;23(21):10.1016/j.bmcl.2013.09.001. doi: 10.1016/j.bmcl.2013.09.001

Table 6.

Head Group SAR

graphic file with name nihms524282u6.jpg
cpd A R1 R2 mGlu5 pIC50 (± SEM)a mGlu5 IC50 (nM) % Glu Max (± SEM)a,b
28 N H 5-F 7.49 ± 0.02 33 1.2 ± 0.2
66 N H 6-CH3 7.75 ± 0.13 18 1.1 ± 0.3
75 N CH3 5-F 5.35 ± 0.04 4470 2.6 ± 0.1
76 N CH3 6-CH3 7.02 ± 0.06 96 1.6 ± 0.2
77 CF H 5-F 7.61 ± 0.04 25 1.1 ± 0.1
78 CF H 6-CH3 8.13 ± 0.08 7.5 1.8 ± 0.4
79 CCN H 5-F 7.57 ± 0.08 27 1.7 ± 0.2
80 CCN H 6-CH3 7.99 ± 0.15 10 1.6 ± 0.1
a

Calcium mobilization mGlu5 assay; values are average of n ≥ 3

b

Amplitude of response in the presence of 30 μM test compound as a percentage of maximal response (100 μM glutamate); average of n ≥ 3