. Author manuscript; available in PMC: 2012 Nov 15.

Published in final edited form as: Bioorg Med Chem Lett. 2011 Sep 20;21(22):6739–6745. doi: 10.1016/j.bmcl.2011.09.049

Table 2. S1P₄–R agonist activity of compounds 19a-19x (EC₅₀ nM).

cpd	Ar	R	R¹	EC50 (nm) ^α
19a	2-chlorophenyl	Me	Me	NA
19b	2-bromophenyl	Me	Me	NA
19c	2-methylphenyl	Me	Me	NA
19d	3-fluorophenyl	Me	Me	1600 (60%) ^β
19e	4-fluorophenyl	Me	Me	433
19f	3-cyano-4-fluoro-phenyl	Me	Me	3200 (50%) ^β
19g	4-methoxy-3-(trifluoromethyl) phenyl	Me	Me	NA
19h	2-methoxy-5-methyl phenyl	Me	Me	NA
19i	2,4-difluorophenyl	Me	Me	210
19j	2,4-dimethylphenyl	Me	Me	NA
19k	4-chloro-2-fluorophenyl	Me	Me	440
19l	phenyl	Et	Et	602
19m	pyridin-2-yl	Me	Me	1800
19n	naphthalen-1-yl	Me	Me	NA
19o	naphthalen-1-yl	Et	Et	NA
19p	3-fluoro-pyridin-2-yl	Me	Me	3100 (70%) ^β
19q	3-fluoro-pyridin-2-yl	Et	Et	5400 (70%) ^β
19r	benzyl	Me	Me	262
19s	2-flurobenzyl	Me	Me	72
19t	2,6-difluorobenzyl	Me	Me	92
19u	2,6-difluorobenzyl	Et	Et	314
19v	2,4-diflurobenzyl	Me	Me	147
19w	1-phenyleth-1-yl	Me	Me	660 (20%) ^β
19x	1-phenyleth-1-yl	Et	Et	NA

^α

Data are reported as mean of n = 3 determinations.

^β

Percentage of response.

NA = not active at concentrations up to 25 μM.

Table 2. S1P4–R agonist activity of compounds 19a-19x (EC50 nM).