Abstract
A recently reported dual LPA 1/LPA 3 receptor antagonist (VPC12249, 1) has been modified herein so as to optimize potency and selectivity at LPA receptors. Compounds containing variation in the acyl lipid chain and linker region have been synthesized and screened for activity at individual LPA receptors. LPA 1-selective ( 14b) and LPA 3-selective ( 10g, m) compounds of modest potency have been discovered. Additionally, 2-pyridyl derivative 10t exhibits a K i value of 18 nM at the LPA 1 receptor and is significantly more potent than 1 at the LPA 3 receptor. This paper describes the synthetic methods, biological evaluation, and structure–activity relationships (SARs) of LPA receptor antagonists.
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