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. Author manuscript; available in PMC: 2012 Dec 1.
Published in final edited form as: Bioorg Med Chem Lett. 2011 Oct 8;21(23):6955–6959. doi: 10.1016/j.bmcl.2011.09.131

Table 2.

SAR of the pyridyl group

graphic file with name nihms334744u2.jpg
Compd R hmGlu4 IC50 (μM)a % Inhibition
2e graphic file with name nihms334744t6.jpg 8.2 ± 0.4 63.1 ± 6.6
3a graphic file with name nihms334744t7.jpg Inactive −3.1 ± 1.3
3b graphic file with name nihms334744t8.jpg Inactive −6.9 ± 3.0
3c graphic file with name nihms334744t9.jpg Inactive −4.0 ± 6.1
3d graphic file with name nihms334744t10.jpg Inactive −1.5 ± 1.5
3e graphic file with name nihms334744t11.jpg Inactive 2.3 ± 1.6
a

Antagonist activity at mGlu4 is assessed by measuring the ability of a compound to concentration-dependently inhibit an EC80 glutamate response. IC50 and % inhibition values are the average of at least three independent determinations (mean ± SEM shown in table). Compounds were ranked as active if they inhibited the EC80 response by at least 20%.