Abstract
Our laboratory has identified several acrylamide derivatives with potent CCR3 inhibitory activity. In the present study, we evaluated the in vitro metabolic stability (CL int; mL/min/kg) of these compounds in human liver microsomes (HLMs), and assessed the relationship between their structures and CL int values. Among the compounds identified, N-{(3 R)-1-[(6-fluoro-2-naphthyl)methyl]pyrrolidin-3-yl}-2-[1-(2-hydroxybenzoyl)piperidin-4-ylidene]acetamide ( 30j) was found to be a potent inhibitor (IC 50 = 8.4 nM) with a high metabolic stability against HLMs.
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