Structural Development Studies of Subtype-Selective Ligands for Peroxisome Proliferator-Activated Receptors (PPARs) Based on the 3,4-Disubstituted Phenylpropanoic Acid Scaffold as a Versatile Template

Table 2

SAR 2: effect of the linker partial structure in the present series of compounds.

		Transactivation activity
		EC50 (nM)^(a)
No.	A	PPAR	PPAR	PPAR
11	CH2NHCO^(c)	40	3600	1000
24	NHCO^(c)	6000	ia^(b)	ia
25	(CH2)2NHCO^(c)	740	1500	ia
26	CH2N(Me)CO^(c)	ia	ia	ia
27	CH2CONH^(c)	130	ia	ia
28	NHCONH^(c)	ia	ia	ia
29	{NHCOC𝛼}^(c)	20	ia	ia
30	CH2CH2CO^(c)	320	ia	7400
31	{CH2CH2C𝛾}^(c)	860	640	ia
32	CH2CH2O^(c)	680	400	ia
33	{CONHC𝛼}^(c)	40	120	10000
34	{CH2NHC𝛾}^(c)	4900	8000	ia

^{(a), (b), (c)} See footnotes of Table 1.