. 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 2.

SAR evaluation of carboxylic acid replacements, 5a-h.

Compound	R¹	R	EC₅₀(μM) hmGluR4^4,^a	% Glu Max
5a	H	H	0.95	104
5b	H	Me	10	106
5c	H	DiMe	Inactive
5d	H	Propyl	9.6	57
5e	H	Cyclopropyl	Inactive
5f	H	Cyclopentyl	Inactive
5g	H	Cyclopropylmethyl	10	80
5h	Morpholine		Inactive
5i			3.3	152

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