. Author manuscript; available in PMC: 2010 Sep 1.

Published in final edited form as: Bioorg Med Chem Lett. 2009 Jul 18;19(17):4967–4970. doi: 10.1016/j.bmcl.2009.07.072

Table 1.

SAR evaluation of the amide substitution, 4a-4i.

Compound	R	EC₅₀ (μM) hmGluR4^4,^a	% Glu Max
2	3,5-dichlorophenyl	0.740	127
4a	3,5-difluorophenyl	inactive
4b	3,5-dimethylphenyl	inactive
4c	3,5- di(trifluoromethyl)phenyl	inactive
4d	3,4-dimethylphenyl	inactive
4e	3-chloro-5-fluorophenyl	2.0	138
4f	3-bromophenyl	inactive
4g	3,4-difluorophenyl	inactive
4h	phenyl	>10	39
4i	benzyl	inactive
4j		inactive
4k	2-pyridyl	inactive
4l	morpholine	inactive
4m	Cyclohexyl	inactive
4n	Cyclobutyl	inactive

Represents the average of at least one experiment performed in triplicate.