Identification and SAR of Glycine Benzamides as Potent
Agonists for the GPR139 Receptor
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Abstract
A focused high throughput screening
for GPR139 was completed for
a select 100K compounds, and new agonist leads were identified. Subsequent
analysis and structure–activity relationship studies identified
(<i>S</i>)-3-chloro-<i>N</i>-(2-oxo-2-((1-phenylethyl)amino)ethyl)benzamide <b>7c</b> as a potent and selective agonist of hGPR139 with an EC<sub>50</sub> = 16 nM. The compound was found to cross the blood–brain
barrier and have good drug-like properties amenable for oral dosing
in rat
